AUTHOR OF THIS BLOG

DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Worlddrugtracker, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India, in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA as ADVISOR earlier GLENMARK LS Research centre as consultant,Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now sSanofi, Searle India ltd, now Rpg lifesciences, etc. he is now helping millions, has million hits on google on all organic chemistry websites. His New Drug Approvals, Green Chemistry International, Eurekamoments in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 year tenure, good knowledge of IPM, GMP, Regulatory aspects, he has several international drug patents published worldwide . He gas good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, polymorphism etc He suffered a paralytic stroke in dec 2007 and is bound to a wheelchair, this seems to have injected feul in him to help chemists around the world, he is more active than before and is pushing boundaries, he has one lakh connections on all networking sites, He makes himself available to all, contact him on +91 9323115463, amcrasto@gmail.com

Scalable Flow Chemistry : A Flexible Tool for the Research, Developments and Production of Pharmaceuticals, Fine & Speciality Chemicals

 FLOW CHEMISTRY, flow synthesis  Comments Off on Scalable Flow Chemistry : A Flexible Tool for the Research, Developments and Production of Pharmaceuticals, Fine & Speciality Chemicals
Oct 072016
 

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Scalable Flow Chemistry : A Flexible Tool for the Research, Developments and Production of Pharmaceuticals, Fine & Speciality Chemicals
– Dr. Charlotte Wiles, Chief Executive Officer, Chemtrix BV, Netherlands

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A PRESENTATION

 

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///////Scalable Flow Chemistry,  A Flexible Tool,  Research, Developments,  Production,  Pharmaceuticals, Fine ,  Speciality Chemicals, Charlotte Wiles, Chief Executive Officer, Chemtrix BV, Netherlands

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11th Pharmacovigilance 2016, 1st Dec 2016, Kohinoor Continental Hotel, Mumbai, India

 CONFERENCE, Uncategorized  Comments Off on 11th Pharmacovigilance 2016, 1st Dec 2016, Kohinoor Continental Hotel, Mumbai, India
Oct 052016
 

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11th Pharmacovigilance 2016

“Ensuring safer drugs to market by analyzing latest developments in pharmacovigilance, drug safety and risk management”

1st December 2016, Kohinoor Continental Hotel, Mumbai, India

After the successful journey of a series of 10 Pharmacovigilance conferences, Virtue Insight is proud to announce its 11th Pharmacovigilance 2016 in India. It is our great pleasure to invite you to the 11th Pharmacovigilance 2016, in Mumbai – India on 1st of December 2016. We have a wide range of scientific topics with something for everyone.

The past is reflected in a session about Indian traditional medicine and the future is discussed under Big Data analytics and in the research of our young scientists. However, we must live and act in the present and debate pressing challenges that face us today in pharmacovigilance (PV). The rates for medication errors are too high. We still struggle to communicate risk well. With the welcome drive towards transparency and respecting human rights, legal and ethical issues in PV have come to the fore. Society’s research enterprise as a whole needs to become far more aware of the commercial reality that PV underpins safety, with its intimate links to innovation, so that safety and must be intrinsically built into successful development and marketing. With governments round the world struggling to curb healthcare costs, the importance of integrating PV into National Health Programmes has never been more important.

It gives me great pleasure in welcoming all of you to the virtue insight’s 11th Pharmacovigilance 2016. I wish and pray that all our efforts will be beneficial to our industries and to our country at large.

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pic KANCHI SHAH, VIRTUEINSIGHT

 

KEY SPEAKERS INCLUDE

JEAN CHRISTOPHE DELUMEAU, Head of Pharmacovigilance Asia-Pacific, Bayer HealthCare (Singapore)

Jean-Christophe Delumeau

 

JESSICA THONGCHAREN, Associate Director Pharmacovigilance, Takeda Pharmaceuticals (Singapore)

 Jessica Thongcharen

ARUN BHATT, Consultant – Clinical Research & Development
V. KALAISELVAN, Principal Scientific Officer, Indian Pharmacopoeia Commission, Ministry of Health & Family Welfare, Govt. of India
SUDHIR PAWAR, Coordinator – ADR monitoring Center at LTMMC & GH, Under Pharmacovigilance Programme Of India (PvPI),Indian Pharmacopoeia Commission
ARUN BHATT, Consultant – Clinical Research & Development
BHASWAT CHAKRABORTY, Senior VP & Chair, Research and Development Core Committee, Cadila
SUTAPA B NEOGI, Additional Professor, Indian Institute of Public Health
DEEPTI SANGHAVI, Assistant Manager – Medical Writing, Tata Consultancy Services
JAMAL BAIG, Country Head – Pharmacovigilance, Merck
SIDDHARTH DESHPANDE, Assistant Professor Department of Clinical Pharmacology, KEM Hospital
ABHAY CHIMANKAR, Head, Global Drug Safety, Cipla
SANDESH SAWANT, Head, Clinical Operations (India and EM), Wockhardt
ABHAY PHANSALKAR, Head Clinical Trials, Cipla
GURPREET SINGH, Head Vendor Management, Drug Safety & Epidemiology, Novartis
MILIND ANTANI, Partner In-Charge – Pharma LifeSciences, Nishith Desai Associates
VARSHA NARAYANAN, Head Medical Affairs, Wockhardt
POOJA JADHAV, Manager, Sun Pharmaceuticals
GODHULI CHATTERJEE, Senior Medical Advisor and Clinical Safety Officer, Sanofi-aventis

Plus Many More..

PEOPLE YOU GET TO MEET

Vice Presidents, Directors, CRO’s, Heads and Managers of:
Pharmacovigilance Strategy, Drug Safety/Risk Management, Information and Clinical Data Management, Clinical Research, Research & Development, Product Safety/Assurance Assessment, Patient Safety & Outcomes Research & Data Analysis, Epidemiology project management, Regulatory Affairs and Compliance, Sales & Marketing, Biotech manufacturers

FROM VARIOUS

Pharmaceutical organizations, Generic pharmaceutical companies, Contract research organizations, Patient recruitment companies, Government- Department of health, Non-profit organizations/ Association, Consultants
This event also serves as a platform for networking opportunities in the relevant field , wherein you get to meet and  broaden  your  contacts to develop your business. We also have sponsorship opportunities available for the event which gives you an opportunity to speak/exhibit and create brand awareness. Or you could even attend the event as a delegate and get a better insight of the updates and  the increasing challenges in the industry . So hurry now and be a part of this massive event.

 

 

GLIMPSES OF MY( DR ANTHONY) INTERACTION

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with Fen Castro of VirtueInsight, Director , and his team , , —thanks for inviting me to 9th Biosimilars Congregation 2016., Lalit hotel, Mumbai, India, 22nd Sept 2016 — with Fen Castro, Kanchi Shahand Virtue Insight at The Lalit Hotel.

 

 

CONFERENCE BOOKING DETAILS

Online Registration http://www.bookmytrainings.com/all-courses/professional-events/event/44991-11th-pharmacovigilance-2016
Early Bird Discount Price – 1 Delegate Pass (INR 6,000 + Tax (15%) – Book and Pay before 17th October 2016 to avail this price
Standard Price (From 18th October 2016) – 1  Delegate Pass – (INR 7,000 + Tax (15%)
Group Discounts (Applicable for 3 or 4) – 1 Delegate Pass  – (INR 6,500 + Tax (15%)
Group Discounts (Applicable for 5 or more) – 1 Delegate Pass  – (INR 6,000 + Tax (15%)
Conference Sponsor & Exhibition Stall – Should you wish to Sponsor, Exhibition Stall (Booth) or a paid Speaker Slot, you can simply call or email your interest and queries to TEL: +91 44 64614333, or sponsor@virtueinsight.com

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REGISTRATION PROCESS

In order to register simply email the below mentioned details to delegate@virtueinsight.com

  • Company Name & Address
  • Attendee Name/Names
  • Job Title
  • Contact Number

We also have some sponsorship opportunities available for the event, which gives you an opportunity to speak/exhibit, and create brand awareness. In addition, the networking opportunities in focused and relevant industry gathering provide the personal contact necessary for business development efforts.

In case you or any of your colleagues might be interested in participating in the same, please let us know and we will be happy to call you and help you with the registration.

 

SEE BROCHURE

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Thank you for your time and consideration.

Fen Castro

Head – Productions

Virtue Insight

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Tel (India) –       + 91 44 64614333

Mobile (India) –  + 91 9003 26 0693

Tel (UK) –          + 44 2036120886

 

 

 

////////////11th Pharmacovigilance,  2016, 1st Dec,  2016, Kohinoor Continental Hotel, Mumbai, India, Conference, fen castro

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Bromoclenbuterol

 Uncategorized  Comments Off on Bromoclenbuterol
Oct 042016
 

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Bromoclenbuterol

Bromoclenbuterol; CAS 37153-52-9; Chlorbrombuterol; AC1MC7W8;
Molecular Formula: C12H18BrClN2O
Molecular Weight: 321.64112 g/mol

 

CLIP

http://dx.doi.org/10.1016/j.chroma.2012.08.031

Volume 1258, 5 October 2012, Pages 55–65

Wide-range screening of banned veterinary drugs in urine by ultra high liquid chromatography coupled to high-resolution mass spectrometry

  • a Center for Public Health Research (CSISP), Avda de Cataluña 21, 46020 Valencia, Spain
  • b Thermo Fisher Scientific, Barcelona, Spain
  • c Analytical Chemistry Department, Universidad de Valencia, Edifici Jeroni Muñoz, 50, Dr. Moliner, 46100 Burjassot, Valencia, Spain

 

CLIP

Synthesis and Characterization of Bromoclenbuterol

Ravi Kumar Kannasani*, Srinivasa Reddy Battula, Suresh Babu Sannithi, Sreenu Mula and Venkata Babu VV

R&D Division, RA Chem Pharma Limited, API, Hyderabad, Telangana, India

*Corresponding Author:
Ravi Kumar Kannasani
R&D Division, RA Chem Pharma Limited
API, Prasanth Nagar, Hyderabad, Telangana, India
Tel: +919000443184
E-mail: kannasani.ravi@rachempharma.com

http://www.omicsonline.org/open-access/synthesis-and-characterization-of-bromoclenbuterol-2161-0444-1000397.php?aid=79341

Citation: Kannasani RK, Battula SR, Sannithi SB, Mula S, Babu VVV (2016) Synthesis and Characterization of Bromoclenbuterol. Med Chem (Los Angeles) 6:546-549. doi:10.4172/2161-0444.1000397

 

4-Amino acetophenone (1) was reacted with N-Chlorosuccinimide in 1N HCl to afford 4-amino-3-chloro acetophenone (7), which was reacted with bromine to give 1-(4-amino-3-bromo-5-chlorophenyl)- 2-bromoethanone (8). The obtained bromo compound was reacted with tertiay -butyl amine to afford 2-(tert-butylamino)-1-(4-amino-3- bromo-5-chlorophenyl)ethanone (9), which was reduced with sodium borohydride in methanol to give bromoclenbuterol compound (10). The synthesized bromoclenbuterol structure was confirmed by 1H NMR, 13C NMR, IR and mass spectra.

1-(4-Amino-3-chlorophenyl)ethanone (7)

To a stirred solution of 1N HCl (1500 ml) was added 4-amino acetophenone (1) (200 gm, 1.48 mole) and N-Chloro succinimide (50 gm, 0.37 mole) at room temperature, and stirring continued for 3 hrs at 25-30°C. After maintenance undissolved material was filtered from the reaction mixture, total filtrate was taken and extracted with ethyl acetate, dried over sodium sulfate and evaporated under vacuum to get crude. Crude material was dissolve in ethyl acetate, titrated with EA-HCl and stirred for 15-30 min to get precipitation. The obtained precipitate was filtered and washed with ethyl acetate, and this acidic titration operation was repeated 2 times to get mono chloro compound as solid material, this solid material was neutralized with sodium carbonate solution in aqueous condition and further purified by using recrystlliaztion technique in ethyl acetate to get 68 gm (yield-27%) 3-chloro-4-amino acetophenone (7) (mono chloro compound), as light brown colored solid with 98.66% HPLC purity (124 gm of unreacted 4-amino acetophenone obtained from aqueous layer).

1-(4-Amino-3-bromo-5-chlorophenyl)-2-bromoethanone (8)

To a stirred solution of 3-chloro-4-amino acetophenone (7) (14 gm, 0.082 mole) in chloroform (140 ml) was added bromine (26.24 gm, 0.164 mole) solution slowly at 25-30°C and stirring continued for 6 hrs at same temperature. After completion of the reaction, methanol was added to the reaction mixture and continued the stirring for 30 min at RT. Undissolved material was filtered, the filtrate was distilled up to 50%, remaining mass was cooled to 0-5°C and filtered to give 15 gm (yield-55%) of 1-(4-amino -3-chloro-5-bromo – phenyl) -2-bromo ethanone (8) as light brown color solid with 95.15% HPLC purity.

2-(Tert-butylamino)-1-(4-amino-3-bromo-5-chlorophenyl) ethanone (9)

To a stirred solution of 1-(4-amino -3-chloro-5-bromo – phenyl) -2-bromo ethanone (8) (8 gm, 0.024 mole) in chloroform (50 ml) was added catalytic amount of potassium iodide (0.1 gm, 0.0006 mole) and tertiary butyl amine (5.2 gm, 0.072 mole) at 0-5°C and stirring was continued for 24 hrs at 0-5°C. After completion of the reaction, undissolved salts were filtered, the filtrate was distilled under vacuum to get crude solid material, which was triturated with hexane to give 6 gm (yield-76%) of 1-(4-amino-3-chloro-5-bromo phenyl)-2-[(1,1- dimethylethyl)amino]ethanone (9) as light pale yellow color solid.

(S)-2-(Tert-butylamino)-1-(4-amino-3-bromo-5- chlorophenyl)ethanol (10)

To a stirred solution of 1-(4-Amino-3-chloro-5-bromo phenyl)- 2-[(1,1-dimethylethyl)amino]ethanone (9) (6 gm, 0.018 mole) in methanol (25 ml) was added sodium borohydride (0.7 gm, 0.018 mole) at 0-5°C. After addition, reaction mixture was slowly allowed to come to room temperature and stirred for 10 hrs at 25-30°C. On completion, reaction mixture was poured in to chilled water, obtained precipitate was filtered, dried and recrystallized in methanol to give 5 gm (yield-82%) of 1RS-1-(4-amino -3-bromo-5-chloro phenyl) -2-[(1,1-dimethyl ethyl)amino ethanol (or) Bromo clenbuterol (10) as off-white solid. HPLC purity-98.80%,

1H NMR (CDCl3): δ 7.35 (d, 1H, J=1.2 Hz), 7.23 (d, 1H, J=1.6 Hz), 4.45 (br s, 2H), 4.42 (dd, 1H, J=9.2, 3.6 Hz), 2.84 (dd, 1H, J=11.6, 3.6 Hz), 2.50 (dd, 1H, J=12.0, 9.2 Hz), 1.10 (s, 9H).

13C NMR (CDCl3): 140.12, 133.93, 128.46, 126.05, 119.16, 109.08, 70.94, 50.33, 50.05, 29.15.

IR (KBr, Cm-1): 3465.99, 3320.19, 2965.04, 1623.40, 1483.88, 1219.17, 758.77, 630.41.

Mass: (m/z)-323.01 (M+2 peak).

 

References

 

 

 

 

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Wanbury successfully completes USFDA inspection at its API facility in Patalganga Plant (01-Oct-2016)

 Uncategorized  Comments Off on Wanbury successfully completes USFDA inspection at its API facility in Patalganga Plant (01-Oct-2016)
Oct 032016
 

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Wanbury has successfully completed US Food and Drug Administration (USFDA) inspection a at its API facility in Patalganga Plant, Maharashtra. The audit was carried out for a period of 4 days from September 26 to September 29, 2016 and concluded successfully. This is the second plant to be approved by USFDA this year, as earlier Tanuku Plant got approval two months ago in July 2016.

Wanbury, one of India’s fastest growing pharmaceutical companies amongst the ‘Top 50 Companies’ in India (as per ORG-IMS), has a strong presence in API global market and domestic branded Formulation. The company’s major thrust area lies in Active Pharmaceutical Ingredient (API) sale in over 70 countries and Pan-India Formulation presence.

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Mr. K. Chandran, Wholetime Director & Vice Chairman

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MR K. CHANDRAN (left), Director, Wanbury, and Mr Asok Shinkar

Patalganga Plant
US FDA approved plant is located at Kaire Village, Taluka: Khalapur, District: Raigad, Maharashtra State. It is situated in Maharashtra Industrial Development Corporation (MIDC), a Govt. notified industrial park for chemical manufacturing. The site is located 80 kilometers south of Mumbai International Airport and is easily accessible by road.

//////////Wanbury, USFDA inspection,  API facility, Patalganga Plant

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Biocatalysis : Biological solutions to a growing world, Pregabalin case study

 drugs  Comments Off on Biocatalysis : Biological solutions to a growing world, Pregabalin case study
Oct 022016
 

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Biocatalysis : Biological solutions to a growing world
– Mr. Michael Foldager, Global Marketing Manager – Biocatalysis, Novozymes A/S, Denmark

Michael Foldager

Michael Foldager

Global Marketing Manager
Novozymes, Copenhagen · Business Development

Copenhagen, Denmark

December 4th, 2015 at “IGCW 2015” in Mumbai. India
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Image result for NovozymesAmerikansk lovgivning holder hånden under Novozymes, når der tales om majsbaseret bioethanol, da det er lovfæstet, at 10 pct. af brændstofforbruget skal kommer fra biobrændstof

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albumedix_albumin_novozmes_synbio_denmark_nottingham_subsidiary_veltis

Animal-free yeast production of Albumin offers huge therapeutic potential in medicine (Source: Albumedix)

 

///////////Biocatalysis, Biological solutions,  growing world, Pregabalin,  case study, Michael Foldager, Global Marketing Manager, Novozymes, Copenhagen

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Enantioselective synthesis of atorvastatin

 Uncategorized  Comments Off on Enantioselective synthesis of atorvastatin
Oct 012016
 

“A simplified catalytic system for direct catalytic asymmetric aldol reaction of thioamides; application to an enantioselective synthesis of atorvastatin”
Kawato, Y.; Iwata, M.; Yazaki, R.; Kumagai, N.; Shibasaki, M.
Tetrahedron 2011, 67, 6539.

A simplified catalytic system for direct catalytic asymmetric aldol reaction of thioamides; application to an enantioselective synthesis of atorvastatin

  • a Institute of Microbial Chemistry, Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan
  • b Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

http://www.sciencedirect.com/science/article/pii/S004040201100799X

Corresponding authors. Tel.: þ81 3 3447 7779; fax: þ81 3 3441 7589 (M.S.); tel.: þ81 3 3441 8133; fax: þ81 3 3441 7589 (N.K.); e-mail addresses: nkumagai@bikaken.or.jp (N. Kumagai), mshibasa@bikaken.or.jp (M. Shibasaki).

atorvastatin as a colorless solid. (54.8 mg, 67% over three steps). Colorless solid;

IR (KBr) n 3410, 2964, 2929, 1731, 1652, 1529, 1508, 1438, 1315, 1241, 1226 cm1 ;

1 H NMR (CD3OD) d 7.30e7.29 (m, 2H), 7.25e7.20 (m, 4H), 7.15e7.13 (m, 2H), 7.11e7.02 (m, 6H), 4.08 (ddd, J¼5.3, 7.8, 16.0 Hz 1H), 4.02e3.98 (m, 1H), 3.91 (ddd, J¼5.3, 7.6, 16.0 Hz, 1H), 3.69e3.63 (m, 1H), 3.40e3.34 (m, 1H), 2.41 (dd, J¼5.2,15.5 Hz,1H), 2.35 (dd, J¼7.6,15.5 Hz,1H),1.75e1.6 (m, 2H), 1.56e1.51 (m, 1H), 1.49 (d, J¼7.1 Hz, 3H), 1.48 (d, J¼7.1 Hz, 3H), 1.47e1.43 (m, 1H);

13C NMR (CD3OD) d 175.9, 169.5, 163.8 ( 1 JCF¼245.5 Hz), 139.9, 139.1, 139.1, 136.4, 134.7 (3 JCF¼7.2 Hz), 131.0, 130.3 (4 JCF¼2.9 Hz),129.6,128.9,126.9,125.2,123.3,121.5,118.1,116.3 ( 2 JCF¼21.6 Hz), 68.6, 67.9, 44.2, 43.3, 42.2, 40.1, 27.7, 22.9, 22.8;

19F NMR (CDCl3) d 113.8; [a]D 23 þ5 (c 0.94, CH3OH);

ESI-MS m/z 581.2 [MþNa]þ; HRMS (ESI) Anal. Calcd for C33FH35N2NaO5 m/z 581.2422 [MþNa]þ, found; 581.2421.

 

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Leveraging GCE for sustainable chemical manufacturing Learning outcomes – Dr. R. Rajagopal, CEO, KnowGenix, India

 Uncategorized  Comments Off on Leveraging GCE for sustainable chemical manufacturing Learning outcomes – Dr. R. Rajagopal, CEO, KnowGenix, India
Sep 302016
 

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Leveraging GCE for sustainable chemical manufacturing Learning outcomes – Dr. R. Rajagopal, CEO, KnowGenix, India

Dr. Rajagopal

Dr. R Rajagopal
Chief Coordinating Officer KnowGenix, INDIA

Dr. Rajagopal COO, KnowGenix, India

Dr. Rajagopal is a Ph.D. Tech from ICT, Mumbai with over two decades of experience in the oil, gas and downstream chemical industry. He coordinates the activities of KnowGenix, a research and growth strategy firm with chemicals, materials energy and carbon advisory practices.

His experience in product research and development of cleaner and inherently safer chemical processes is complemented by his industrial experience in process optimization, production planning, manufacturing, and projects management. He now researches micro and macro level trends in the chemicals, materials and energy sectors to provide insights on markets, technology, economics and sustainable processes.

Besides authoring over 100 technical and business reports, he has co-authored the book, “Environmental Perspectives of Chemical Industry: Socio-Economic and Technological Imperatives”, (1993) with Dr. S. B. Chandalia, Former Director, ICT. He was chosen as the “2008-09 Pidilite Industry Visiting Fellow” by ICT, Mumbai. He conducts courses on “Design and Development of Inherently Safer Organic Chemical Processes” and “Green Chemistry and Technology: Design and Development Strategies” to B.Tech. students and industry professionals.

He is actively involved in rural education and technology initiatives and in particular, renewable energy resources providing resource management expertise. Dr. Rajagopal is also associated with Centre for Management Technology, Singapore, as its Director, India, and with Chemical Weekly, Mumbai, as its Consulting Editor, since 1996.

Dr. Rajagopal’s Abstract for IGCW 2011

Summary

Raj is the founder of KnowGenix, a growth strategy firm involved in chemical, material and energy practices. KnowGenix assists clients with growth strategy services through customized, competitive and timely solutions covering Asia, M.E., EU and US geographies in collaboration with its global partners.

Specialties:
His areas of expertise include strategic consulting, business research, technology analysis and capacity building. As a strategy advisor he is now active in assisting companies in business diversification, customer engagement models, portfolio rationalization, structuring alliances, and sustainability practices.

His present research covers technology, regulatory and sustainability trends in chemical, energy, and natural resource sectors.

Experience

Founder & Chief Coordinating Officer

Knowgenix

– Present (13 years 9 months)Mumbai

Growth strategy consulting in chemicals, materials and energy sectors.

Advisor – Editorial

Chemical Weekly

(17 years 9 months)Mumbai Area, India

Chemical Weekly is India’s largest Chemical industry magazine. Raj is associated with the company as an Editorial advisor.

Founder & Chief Coordinating Officer

Knowgenix

(8 years 8 months)B-602, Godrej coliseum, K.J.Somaiya Hospital Road, Sion [E] Mumbai400022

Raj researches business and technology trends in petrochemicals, fine, specialty and life science chemicals value chain as well as in materials and energy.

Raj has over two decades of experience in the chemical value chain. His experience in product research and development of cleaner and inherently safer chemical processes is complemented by expertise in process optimization, production planning, manufacturing, and projects management.

University of Mumbai

Ph.D. Tech., Chemical Technology

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Azaspiracid-1

 Uncategorized  Comments Off on Azaspiracid-1
Sep 302016
 
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 Azaspiracid-1: sc-202482...
AZA-1
Application:An activator of JNK and cell growth inhibitor
CAS Number:214899-21-5
Molecular Weight:842.1
Molecular Formula:C47H71NO12
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Thivisha Rajagopal 
Thivisha Rajagopal

Thivisha Rajagopal scored 13 on the Biological Sciences and 12 on the Physical Sciences sections of the MCAT. Thivisha has completed a B. Sc. in Medicinal Chemistry and an M.Sc. in Chemistry. Thivisha is passionate about teaching Organic Chemistry and she has been a Teaching Assistant for Organic Chemistry I and II for the past two and half years. Thivisha has also been tutoring students in General Chemistry, Organic Chemistry, and Biochemistry for over 10 years. In the classroom, Thivisha is very informal and likes to build a healthy and comfortable relationship with students. She believes it is very important to allow students to interact in discussion with their peers and the teacher.

Education

2010, M.Sc. [Chemistry]
2007, B.Sc. (Honours) [Medicinal Chemistry]

Teaching Experience

2009-Present, Lecturer, Chemistry
2009-Present, Lecturer, Biology
2008-10, Lecture TA, Organic Chemistry
2007-8, Lab TA, Organic Chemistry
1999-2010, Private Tutor, General Chemistry, Organic Chemistry, Biochemistry

Thivisha RajagopalEmail: traja085@hotmail.com

Department of Chemistry, University of Ottawa, 10 Marie Curie, Ottawa, ON, K1N 6N5, Canada

Azaspiracid-1 is an activator of JNK (c-Jun-N-terminal kinase)and caspases. It is a cellular growth inhibitor and inducer of cytoskeletal alterations. Azaspiracid-1 is also a modulator of intracellular cAMP (cyclic adenosine monophosphate) and calcium levels. It acts as an inhibitor of cholesterol biosynthesis in human T lymphocyte cells. Azaspiracid-1 is a potent teratogen to finfish and also acts as a cytotoxin to mammalian cells. 

References

Multiple organ damage caused by a new toxin azaspiracid, isolated from mussels produced in Ireland: E. Ito, et al.; Toxicon 38, 917 (2000) Azaspiracid-1, a potent, nonapoptotic new phycotoxin with several cell targets: Y. Roman, et al.; Cell. Signal. 14, 703 (2002) Teratogenic effects of azaspiracid-1 identified by microinjection of Japanese medaka (Oryzias latipes) embryos: J.R. Coleman, et al.; Toxicon 45, 881 (2005) Cytotoxic and cytoskeletal effects of azaspiracid-1 on mammalian cell lines: M.J. Twiner, et al.; Toxicon 45, 891 (2005) Azaspiracids modulate intracellular pH levels in human lymphocytes: A. Alfonso, et al.; BBRC 346, 1091 (2006) Cell growth inhibition and actin cytoskeleton disorganization induced by azaspiracid-1 structure-activity studies: N. Vilarino, et al.; Chem. Res. Toxicol. 19, 1459 (2006) The c-Jun-N-terminal kinase is involved in the neurotoxic effect of azaspiracid-1: C. Vale, et al.; Cell Physiol. Biochem. 20, 957 (2007) Effects of azaspiracid-1, a potent cytotoxic agent, on primary neuronal cultures. A structure-activity relationship study: C. Vale, et al.; J. Med. Chem. 50, 356 (2007) Irreversible cytoskeletal disarrangement is independent of caspase activation during in vitro azaspiracid toxicity in human neuroblastoma cells: N. Vilarino, et al.; Biochem. Pharmacol. 74, 327 (2007) Transcriptional profiling and inhibition of cholesterol biosynthesis in human T lymphocyte cells by the marine toxin azaspiracid: M.J. Twiner, et al.; Genomics 91, 289 (2008)

 

Total Synthesis of (+)-Azaspiracid-1. An Exhibition of the Intricacies of Complex Molecule Synthesis

Department of Chemistry & Chemical Biology, Harvard University, Cambridge, Massachusetts 02138
J. Am. Chem. Soc., 2008, 130 (48), pp 16295–16309
DOI: 10.1021/ja804659n

 

Abstract Image

The synthesis of the marine neurotoxin azaspiracid-1 has been accomplished. The individual fragments were synthesized by catalytic enantioselective processes: A hetero-Diels−Alder reaction to afford the E- and HI-ring fragments, a carbonyl-ene reaction to furnish the CD-ring fragment, and a Mukaiyama aldol reaction to deliver the FG-ring fragment. The subsequent fragment couplings were accomplished by aldol and sulfone anion methodologies. All ketalization events to form the nonacyclic target were accomplished under equilibrating conditions utilizing the imbedded configurations of the molecule to adopt one favored conformation. A final fragment coupling of the anomeric EFGHI-sulfone anion to the ABCD-aldehyde completed the convergent synthesis of (+)-azaspiracid-1.

str1 str2

(+)-azaspiracid-1 (ent-2) (5.4 mg, 90%) as a white solid. TLC Rf = 0.25 (25:75 MeOH/EtOAc);

[α] 24 D +21.7 (c 1.00, MeOH);

IR (film) 3301, 3175, 3000 (br), 2957, 2927, 2872, 1774, 1731, 1581, 1459, 1439, 1408, 1379, 1318, 1267, 1242, 1223, 1199, 1143, 1127, 1069, 1044, 1023, 984, 875, 862, 840, 805, 734 cm−1 ;

1 H NMR (600 MHz, CD3OD, AcOH added) δ 5.78-5.71 (m, 2H, C8H, C4H), 5.64 (bd, 1H, J = 10 Hz, C7H), 5.47 (dd, 1H, J = 15, 7 Hz, C5H), 5.36 (d, 1H, J = 1 Hz, C44Ha), 5.18 (d, 1H, J = 2 Hz, C44Hb), 5.03 (t, 1H, J = 4 Hz, C34H), 4.81 (app bd, J = 2 Hz, C6H), 4.43 (td, 1H, J = 9, 6 Hz, C19H), 4.37 (bd, 1H, J = 3.5 Hz, C32H), 4.24 (bs, 1H, C17H), 4.09 (d, 1H, J = 3 Hz, C33H), 4.00 (d, 1H, J = 10 Hz, C25H), 3.93 (d, 1H, J = 5.5 Hz, C20H), 3.91 (bd, 1H, J = 2 Hz, C16H), 2.91 (bdd, 1H, J = 12, 3 Hz, C40Ha), 2.83 (t, 1H, J = 12 Hz, C40Hb), 2.66 (dd, 1H, J = 15, 4.5 Hz, C35Ha), 2.50 (d, 1H, J = 15 Hz, C35Hb), 2.51-2.47 (m, 1H, C9Ha), 2.43 (d, 1H, J = 14 Hz, C27Ha), 2.37-2.30 (m, 5H, C3H2, C11Ha, C2H2), 2.26 (d, 1H, J = 14 Hz, C27Hb), 2.27-2.22 (m, 1H, C30H), 2.19-2.09 (m, 3H, C12Ha, C9Hb, C22H), 2.09-1.95 (m, 6H, C29Ha, C14H, C18H2, C37H, C12Hb), 1.93-1.89 (m, 1H, C39H), 1.88-1.83 (m, 2H, C31Ha, C15Ha), 1.76 (app dt, 1H, J = 14, 3 Hz, C15Hb), 1.72-1.69 (m, 1H, C38Ha), 1.68 (dd, 1H, J = 12, 7 Hz, C11Hb), 1.53 (dt, 1H, J = 13.5, 5 Hz, C31Hb), 1.46-1.42 (m, 2H, C23H2), 1.40-1.27 (m, 3H, C29Hb, C24H, C38Hb), 0.99 (d, 3H, J = 7 Hz, C46H3), 0.97 (d, 6H, J = 6 Hz, C45H3, C47H3), 0.96 (d, 3H, J = 6 Hz, C41H3), 0.92 (d, 3H, J = 7 Hz, C42H3), 0.85 (d, 3H, J = 7 Hz, C43H3);

13 C NMR (125 MHz, CD3OD, AcOH added) δ 177.8 (C1), 148.4 (C26), 132.4 (C4H), 131.4 (C5H), 129.2 (C7H), 123.4 (C8H), 117.0 (C44H2), 111.3 (C13), 107.2 (C10), 100.2 (C21H), 98.7 (C28), 96.7 (C36), 81.6 (C33H), 79.6 (C25H), 79.1 (C19H), 78.2 (C16H), 76.7 (C20H), 74.8 (C34H), 73.3 (C17H), 72.8 (C32H), 72.3 (C6H), 49.2 (C27H2), 46.1 (C40H2), 44.1 (C29H2), 42.4 (C24H), 41.7 (C35H2), 38.2 (C23H2), 37.6 (C38H2), 37.5 (C12H2), 37.2 (C18H2), 36.7 (C22H), 35.7 (C9H2, C37H), 35.30, 35.25 (C2H2, C31H2), 33.2 (C11H2), 32.6 (C15H2), 30.9 (C14H), 29.3 (C3H2), 29.0 (C39H), 26.3 (C30H), 23.5 (C45H3), 18.5 (C47H3), 18.1 (C43H3), 16.6 (C41H3), 16.4 (C42H3), 15.5 (C46H3); Exact mass calcd for C47H71NO12 ([M+H] + ): 842.5054; found: 842.5023 (ESI).

http://pubs.acs.org/doi/suppl/10.1021/ja804659n/suppl_file/ja804659n_si_001.pdf

//////////Structural Elucidation, Total Synthesis , Azaspiracid-1,  Thivisha Rajagopal,  January 29, 2009,  University of Ottawa

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Pharmaron to acquire Merck Sharpe & Dohme’s Hoddesdon research facility in UK

 companies  Comments Off on Pharmaron to acquire Merck Sharpe & Dohme’s Hoddesdon research facility in UK
Sep 302016
 

 

Pharmaron to acquire Merck Sharpe & Dohme’s Hoddesdon research facility in UK
Pharmaron has signed a non-binding heads of terms with Merck Sharpe & Dohme Limited (MSD) for the purchase of UK-based Hoddesdon site, which comprises MSD’s process development and research facility.

read at

http://www.pharmaceutical-technology.com/news/newspharmaron-to-acquire-merck-sharpe-dohmes-hoddesdon-research-facility-in-uk-5015533?WT.mc_id=DN_News

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HODDESDON – Company Headquarters and Pharmaceutical Research and development Laboratories (PR&D). MSD has been present in Hoddesdon since the 1940s.

September 26, 2016 05:00 AM Eastern Daylight Time

BEIJING–(BUSINESS WIRE)–Pharmaron has entered into a non-binding Heads of Terms (HoTs) with Merck Sharpe & Dohme Limited (MSD) for the sale of the Hoddesdon UK site which includes MSD’s process development and research facility. The parties hope to complete the deal in Q1 2017.

Pharmaron and MSD agree deal to acquire MSD’s UK Hoddesdon site

Pharmaron sees this as a unique opportunity to acquire state-of-the-art Good Manufacturing Practice (GMP) standard facilities for the development of Active Pharmaceutical Ingredients (API) and formulation development in Europe to complement Pharmaron’s existing world class chemistry and integrated drug discovery and development services globally. Under the deal, MSD will remain on site on and lease-back the main office buildings.

Louise Houson, Managing Director, MSD UK and Ireland commented: “We are very pleased to be progressing this deal with Pharmaron. This deal will secure the future of the site while meeting the changing business needs of MSD and its employees for the foreseeable future. It also ensures MSD’s scientific legacy in Hoddesdon continues, with the potential to create local opportunities for our scientific staff in their areas of expertise.”

Boliang Lou, Chairman and CEO of Pharmaron commented that: “This is an exciting opportunity to have an industry-leading R&D site join the Pharmaron group, which once again demonstrates our commitment to our mission to become a world leader in small molecule drug R&D services. It allows us to develop our global capabilities in process chemistry and manufacturing services area, strengthening our capabilities in fully integrated R&D services. Together with the recent addition of GMP radiochemistry and GCP/GLP metabolism platforms through acquisition of Quotient Bioresearch in the U.K., this deal further consolidates our strategic position in Europe to better serve our partners globally, particularly in Europe.”

Commercial details on the transaction are not being disclosed.

About Pharmaron
Pharmaron is a private, premier R&D service provider for the life science industry. Founded in 2003, Pharmaron has invested in its people and facilities, and established a broad spectrum of drug R&D service capabilities, ranging from synthetic and medicinal chemistry, biology, DMPK, pharmacology, safety assessment, radiochemistry and radiolabelled metabolism to chemical & pharmaceutical development. With about 4,000 employees and operations in China, the U.S. and the U.K., Pharmaron has an excellent track record in the delivery of R&D solutions to its partners in North America, Europe, Japan and China. For more information, please visit: www.pharmaron.com

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About MSD
For 125 years, MSD has been a global healthcare leader working to help the world be well. MSD is a trade name of Merck & Co., Inc., Kenilworth, NJ., USA. Through our prescription medicines, biologic therapies, and animal health products, we work with customers and operate in more than 140 countries to deliver innovative health solutions. We also demonstrate our commitment to increasing access to healthcare through far-reaching policies, programmes and partnerships. For more information, visit www.msd-uk.com.

//////Pharmaron,  Merck Sharpe & Dohme,  Hoddesdon research facility,  UK

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Dr. D. Srinivasa Reddy of NCL receives the Shanti Swarup Bhatnagar Prize New Delhi, India

 Uncategorized  Comments Off on Dr. D. Srinivasa Reddy of NCL receives the Shanti Swarup Bhatnagar Prize New Delhi, India
Sep 292016
 

 

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Dr. D. Srinivasa Reddy of NCL receives the Shanti Swarup Bhatnagar Prize New Delhi, India

Dr. D. Srinivasa Reddy
Senior Scientist
Organic Chemistry Division
National Chemical Laboratory
PUNE, INDIALINKS
 

 NCL PUNE INDIA

 WEBSITE–http://www.ncl-india.org/

Dr. Srinivasa Reddy of CSIR-NCL bags the prestigious Shanti Swarup Bhatnagar Prize

The award comprises a citation, a plaque, a cash prize of Rs 5 lakh

dr

The Shanti Swarup Bhatnagar Prize for the year 2015 in chemical sciences has been awarded to Dr. D. Srinivasa Reddy of CSIR-National Chemical Laboratory (CSIR-NCL), Pune for his outstanding contributions to the area of total synthesis of natural products and medicinal chemistry.
This is a most prestigious award given to the scientists under 45 years of age and who have demonstrated exceptional potential in Science and Technology. The award derives its value from its rich legacy of those who won this award before and added enormous value to Indian Science.
Dr. Reddy will be bestowed with the award at a formal function, which shall be presided over by the honourable Prime Minister. The award, named after the founder director general of Council of Scientific & Industrial Research (CSIR), Dr. Shanti Swarup Bhatnagar, comprises a citation, a plaque, a cash prize of Rs 5 lakh.
Dr. Reddy’s research group current interests are in the field of total synthesis and drug discovery by applying medicinal chemistry. He has also been involved in the synthesis of the agrochemicals like small molecules for crop protection. The total synthesis of more than twenty natural products has been achieved in his lab including a sex pheromone that attracts the mealy bugs and has potential use in the crop protection. On the medicinal chemistry front significant progress has been made by his group using a new concept called “Silicon-switch approach” towards central nervous system drugs. Identification of New Chemical Entities for the potential treatment of diabetes and infectious diseases is being done in collaboration with industry partners.
His efforts are evidenced by 65 publications and 30 patents. He has recently received the NASI-Reliance industries platinum jubilee award-2015 for application oriented innovations and the CRSI bronze medal. In addition, he is also the recipient of Central Drug Research Institute award for excellence in the drug research in chemical sciences and scientist of the year award by the NCL Research Foundation in the year 2013. Dr. Reddy had worked with pharmaceutical companies for seven years before joining CSIR-NCL in 2010.

His team

 

//////////Dr. D. Srinivasa Reddy,  NCL, Shanti Swarup Bhatnagar Prize,  PM, Narendra Modi,

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