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

An efficient way for the N-formylation of amines by inorganic-ligand supported iron catalysis

 organic chemistry, SYNTHESIS  Comments Off on An efficient way for the N-formylation of amines by inorganic-ligand supported iron catalysis
Jan 162020
 

Graphical abstract: An efficient way for the N-formylation of amines by inorganic-ligand supported iron catalysis

 

An efficient way for the N-formylation of amines by inorganic-ligand supported iron catalysis

Green Chem., 2020, Advance Article

DOI: 10.1039/C9GC03564H, Paper
Zhikang Wu, Yongyan Zhai, Wenshu Zhao, Zheyu Wei, Han Yu, Sheng Han, Yongge Wei
A green and highly efficient N-formylation of amines using formic acid as the acylating agent by iron catalysis with excellent selectivity and yields.
To cite this article before page numbers are assigned, use the DOI form of citation above.
The content of this RSS Feed (c) The Royal Society of Chemistry

An efficient way for the N-formylation of amines by inorganic-ligand supported iron catalysis

 Author affiliations

Abstract

The first example of an inorganic-ligand supported iron(III) catalysed coupling of formic acid and amines to form formamides is reported. The pure inorganic catalyst (NH4)3[FeMo6O18(OH)6] (1), which consists of a central FeIII single-atomic core supported within a cycle-shaped inorganic ligand consisting of six MoVIO6 octahedra, shows excellent activity and selectivity, and avoids the use of complicated/commercially unavailable organic ligands. Various primary amines and secondary amines have been successfully transformed into the corresponding formamides under mild conditions, and the formylation of primary diamines has also been achieved for the first time. The Fe catalyst 1 can be reused several times without appreciable loss of activity.

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Image result for Zhikang Wu School of Chemical and Environmental Engineering Shanghai Institute of Technology, No. 100 Haiquan Road, Shanghai 201418, P.R. China

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Panthera Deluxe, Polymeric spe products from Orochem

 Uncategorized  Comments Off on Panthera Deluxe, Polymeric spe products from Orochem
Nov 302019
 

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Polymer-based Solid Phase Extraction Products

Orochem synthesizes a full range of polymer-based, solid phase extraction (SPE) sorbents. Every sorbent batch must pass a series of quality control tests to ensure batch-to-batch reproducibility and performance.  Orochem’s Panthera Deluxe and Agility Deluxe products provide high performance at an affordable price.  Sorbents are available in cartridges, 96-well plates, and microelute plate format. Combined method development 96-well plates can be custom made upon request.

Panthera Deluxe Polymeric SPE Products

The Panthera Deluxe sorbent is based on poly-DVB and provides both hydrophobic and hydrophilic retention. It demonstrates high capacity and retention for a full range of neutral, basic, and acidic compounds and is particularly suitable for pain management drugs and other pharmaceuticals.

Technical Specifications:

Mode: Reversed phase

Average Particle Size: 15 µm

Average Pore Size: 39 Å

Sorbent Substrate: Polymeric DVB

Water Wettable: Yes

Mass Spec Compatible:  Yes

pH Range: 0-14

 

Orochem customers have used Panthera Deluxe to separate the following examples in various matrices:

  • Reloxifene
  • Albendazole
  • Topiramate
  • Pregabalin
  • Dolutegravir
  • Dapagliflozine
  • Ibuprofen
  • Loratidine
  • Bile Acids
  • Paliperidon
  • Sofosbuuvir
  • Chlorozoxazone
  • Pramipexole
  • Hydroxychloroquine
  • Isosorbide Mononitrate
  • Bupivacaine Liposomal
  • Amphotericine B Liposomal

 

General Extraction Method

(based on 30 mg/cc cartridge)

Stationary phase: Reversed phase

(Panthera Deluxe )

Condition(optional): 1 ml of methanol followed by 1 ml of water

Loading step: 0.1-0.5 ml of plasma or other sample

Washing step: 1 ml of water followed by 1 ml of 5% methanol (depending on analyte)

Elution step: 1 ml of methanol (depending on analyte, other common solvents are acetonitrile, ethanol)

 

 

A PRESENTATION

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Dr. June Zang
Orochem Technologies Inc. , USA
Tel: 001 -630 210 8300
Dr. Ganesh Metangale
Orochem India Pvt. Ltd.
Tel: 022-20873568/70/71
Orochem Technologies Inc.
Nepervill

Established in 1996, Orochem Technologies Inc. started as a Biotech and Chromatography company to manufacture unique Sample Prep Technology “Products” for the Bioanalysis, Drug Discovery, and the Genomics and Proteomics markets.

Established in 1996, Orochem Technologies Inc. started as a Biotech and Chromatography company to manufacture unique Sample Prep Technology Products for the Bioanalysis, Drug Discovery, and the Genomics and Proteomics markets. Backed with unique expertise in high throughput formats, membranes and surface chemistries, Orochem was one of the first companies to translate the concept of pre-filters from single to high throughput formats, a concept now widely implemented for sample prep plates in the biotech and analytical markets. In the year 2001 Orochem manufactured the first commercially available Protein Crash and Precipitation 96-well plate for Bioanalytical processes. By the year 2006, with the acquisition of Column Engineering Inc, Orochem evolved to become a “full-service” provider for silica manufacturing utilized for analytical and preparatory chromatography. Orochem invests heavily into R&D in-house and owns strong intellectual property in stationary phases for achiral and Chiral Chromatography.

Orochem’s is globally recognized as an organization that conceives, develops, and installs some of the most technologically viable solutions for “highest purities” for industrial or “metric ton” scale purification for API’s, nutritional supplements, fatty acids, and specialty sugars. Orochem provides Simulated Moving Bed (SMB) Chromatography technology for the laboratory scale, pilot scale and large-scale purification of commercially viable molecules for its customers around the world. Orochem’s products and services for Simulated Moving Bed Chromatography include Synthesis and manufacture of stationary phases “tailored for specific separations”, a uniquely engineered SMB system and the installation and commissioning of the SMB systems at customer sites with well-trained Orochem technical service engineers.

Orochem owns several manufacturing facilities around the world. The  Naperville, Illinois, USA site has about 84,000 square feet of manufacturing area where most of the Membrane Filter Plates, Silica manufacturing, Silica bonding, Solid Phase Extraction products and HPLC Columns are manufactured. Orochem India, Mumbai has 20,000 square feet facility and manufactures Sample prep products for the Discovery & Clinical Research organizations in Asia. Simulated Moving Bed chromatography systems are designed, built and assembled completely at our US locations in Naperville in Illinois.

USA (HQ)

Orochem Technologies Inc.
   630 210 8300
   630 210 8315
   info@orochem.com
   340 Shuman Blvd., Naperville, 60563, IL.

Orochem Molecular Purification by Design

https://orochem.com/

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AGGARWWAL EXPORTS : R-Glycidyl Butyrate first in India

 MANUFACTURING, SYNTHESIS, Uncategorized  Comments Off on AGGARWWAL EXPORTS : R-Glycidyl Butyrate first in India
Nov 222019
 

 

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Aggarwwal Exports becomes first company in India  to manufacture R-Glycidyl Butyrate (CAS No. :  60456-26-0) in India. The company holds a GMP and US FDA registration for the product with an audit ready plant.

Aggarwwal Exports – Specialty chemical division’s core strength is Chiral Molecules. R-Glycidyl Butyrate is a Linezolid intermediate that is either imported from China or South Korea, until now.  As China’s reliablility due to Trade War and pollution problems have arisen, more companies are looking to develop Indian Manufacturers to ensure longevity and robustness of Raw Material Supply.

The company has developed a process from the base level of Racemic Epichlorohydrin and is utilizing precious metal to create chirally pure S-Epichlorohydrin and R-Epichlorohydrin, which is further processd to make R-Glycidyl Butyrate and R-Glycidol.

Benefits of purchasing from Aggarwwal Exports-

1) 99% GC purity and 99% Chiral Purity

2) Importing from China and Japan is a tedious process as import duty needs to be made, lead time is around 2 months as R-GB is under Hazardous cargo which is expensive to ship.

3) Pricing is slightly lower than imports but quality is improved.

4) Lead time is 10 days from order confirmation.

5) Most importantly, Make in India.str1.JPG str2 str3 str4

Pranjal Varshney, V.P. Operations

www.agexpharma.com                                        

Aggarwwal Exports, B-8 Roshan Bagh, Rampur 244901 (UP) India

Cell: +91-9837035981 | Email: Pranjal@agexpharma.com

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Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant

 green chemistry, spectroscopy, SYNTHESIS, Uncategorized  Comments Off on Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant
Oct 152019
 

Graphical abstract: Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant

An efficient synthetic approach for the synthesis of α-pyrones via Baeyer–Villiger-type oxidation of α-iodocyclopentenones through a catalyst- and additive-free system using air as an environmentally benign oxidant is described. The reaction exhibits excellent functional group compatibility and provides a simple and efficient protocol for the construction of highly functionalized α-pyrones under mild reaction conditions.

Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant

 Author affiliations

http://www.rsc.org/suppdata/c9/gc/c9gc02725d/c9gc02725d1.pdf

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Catalyst- and Additive-Free Baeyer−Villiger-type Oxidation of α-Iodocyclopentenones to α-Pyrones: Using Air as the Oxidant

 ANTHONY CRASTO, organic chemistry, spectroscopy, SYNTHESIS  Comments Off on Catalyst- and Additive-Free Baeyer−Villiger-type Oxidation of α-Iodocyclopentenones to α-Pyrones: Using Air as the Oxidant
Sep 112019
 

Catalyst- and Additive-Free Baeyer−Villiger-type Oxidation of α-Iodocyclopentenones to α-Pyrones: Using Air as the Oxidant

Abstract

An efficient synthetic approach for the synthesis of α-pyrones via Baeyer−Villiger-type oxidation of α-iodocyclopentenones through a catalyst- and additive-free system using air as an environmentally benign oxidant is described. The reaction exhibits excellent functional group compatibility and provides a simple and efficient protocol for the construction of highly functionalized α-pyrones under mild reaction conditions.

Ethyl 4-(4-cyclopropyl-2-oxo-2H-pyran-6-yl)butanoate (2aa) Product 2aa was obtained as yellow oil in 50% yield (38 mg) following the general procedure; 1H NMR (600 MHz, CDCl3) δ 5.84 (s, 1H), 5.61 (s, 1H), 4.13-4.09 (m, 2H), 2.48 (t, J = 7.3 Hz, 2H), 2.33 (td, J = 7.3, 2.3 Hz, 2H), 1.97-1.94 (m, 2H), 1.66-1.63 (m, 1H), 1.26-1.22 (m, 3H), 1.07-1.05 (m, 2H), 0.80-0.79 (m, 2H); 13C NMR (150 MHz, CDCl3) δ 172.8, 163.9, 163.0, 162.8, 106.7, 102.1, 60.5, 33.2, 33.0, 22.1, 15.4, 14.2, 10.0; HRMS (ESI) calcd. for C14H18O4Na [M+Na]+ : 273.1097, found: 273.1101

 

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https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

http://www.rsc.org/suppdata/c9/gc/c9gc02725d/c9gc02725d1.pdf

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EP Patent Validation Service

 PATENTS, Uncategorized  Comments Off on EP Patent Validation Service
Sep 062019
 

EP Patent Validation Service

Sandeep Mishra

Director at De Science Infoware Pvt Ltd

Traditional route

The conventional route for EP patent validation is for the client to instruct their EP attorneys to execute the validation. The EP attorneys would then instruct a validations provider (like us) or perform the validations themselves using attorney partners in each country who they use based on a reciprocity model, which is usually not cost or quality selective. The EP attorneys would add significant fees for each country.

About our EP Patent Validation service : Why you should go with us.

Benefits of using our EP validation service :

By using a centralised validations provider like us, the client is cutting out one extra layer of cost, which is usually the most significant cost layer. All large patent filers in Europe use a centralised provider like our associate company because of benefits like the following:

Reduced Risk

We with our European team are specialists in European Patent Validation, which means there is a significantly reduced risk of misunderstanding, unexpected costs, or of course the unthinkable risk of accidental loss of a patent due to the complex and constantly changing regulations around Europe.

Reduced Cost

Validation is a significant part of the cost of a European Patent lifecycle, especially if many countries are required. Filing tens of thousands of validations per year, and translating millions of words into every language, means that ours buying power is enormous. We provide user-friendly and extremely efficient processes to our agents and suppliers which further reduce their costs, and all of this means we are able to pass on these savings to our customers.

We expect to able to reduce most client’s validations costs by at least 50%

s

Sandeep Mishra

Director at De Science Infoware Pvt Ltd

Sandeep’s Profile
Website  descienceinfoware  (Company Website)
Phone
+91 8953745897 (Work)
Email
sandeepm@scienceinfoware.com, 

///////////Sandeep Mishra, Director, e Science Infoware, ep, patent

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Engineering of a fungal laccase to develop a robust, versatile and highly-expressed biocatalyst for sustainable chemistry

 Uncategorized  Comments Off on Engineering of a fungal laccase to develop a robust, versatile and highly-expressed biocatalyst for sustainable chemistry
Sep 042019
 

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Engineering of a fungal laccase to develop a robust, versatile and highly-expressed biocatalyst for sustainable chemistry

Abstract

Fungal laccases can play an important role as biocatalysts in organic chemistry to replace chemical synthesis. In a previous work we synthesized conductive polyaniline using a high-redox potential laccase from our collection of recombinant fungal variants. Still, the oxidation of aniline is hindered by the reaction conditions (low pH and presence of anionic surfactants). Thus, we tackle here the directed evolution of the enzyme asisted by computational simulation aiming at improving aniline oxidation at the required polymerization conditions while maintaining the enzyme´s substrate promiscuity. Simultaneously, its secretion by the host used for the engineering (Saccharomyces cerevisiae) was enhanced. Then, the improved laccase variant was overproduced in the industrial host Aspergillus oryzae and assayed for one‐pot synthesis of polyaniline and naphtol-derived dyes whose textile dyeing properties were verified in an industrial environment. Finally, modification of its C-terminal tail further enhanced laccase stability by flexibilization of the region. The resulting biocatalyst displays noticeable stability at high temperature and extreme pH while shows improved kcat values on the different substrates tested. Moreover, it is remarkably produced in S. cerevisiae at rates not formerly reported in the literature. These facts, together with the overexpression in A. oryzae opens new scenarios for its further development and application.

Enzyme production and purification Laccase was produced by S. cerevisiae 1 L-flask cultures and purified as described before.5 Laccase activity in the culture was measured spectrophotometrically with 3 mM ABTS in 100 mM citrate-phosphate buffer, pH 3 by the increase of Absorbance 418 nm (ε418 = 36000 M−1 cm−1). One activity unit (U) was defined as the amount of enzyme needed to transform 1 µmol substrate/minute. To estimate enzyme production, enzyme concentration of a purified laccase variant was measured by the A280 (Nanodrop 2000, Thermofisher, USA) and the specific activity (U/mg) was calculated and used to deduce the mg of enzyme/l obtained in the culture. Enzyme characterization All characterization assays were performed with purified enzymes.

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https://pubs.rsc.org/en/content/articlepdf/2019/gc/c9gc02475a

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Towards cleaner PolarClean: efficient synthesis and extended applications of the polar aprotic solvent methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate

 green chemistry  Comments Off on Towards cleaner PolarClean: efficient synthesis and extended applications of the polar aprotic solvent methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate
Jul 302019
 

Graphical abstract: Towards cleaner PolarClean: efficient synthesis and extended applications of the polar aprotic solvent methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate

Abstract

As a result of recent efforts in green solvent selection, methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate, sold under the brand name Rhodiasolv PolarClean, has received considerable scientific and industrial attention as a possible non-toxic replacement for common polar aprotic solvents. However, the multicomponent nature and multi-step synthesis of this solvent remains an obstacle for its more widespread use and niche applications. In this work, a retrosynthetic approach was taken to identify novel shorter synthetic routes in alignment with green chemistry principles. High purity methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate was obtained in novel single-step reactions via two different base-catalysed Michael additions from readily available building blocks. The more advanced synthetic route shows great potential owing to the swift (30 min), solvent-free reaction and catalytic amounts of base (<6.5 mol%). Green metrics analysis, including Atom Economy, Complete E factor, Carbon Intensity and hazard analysis found the new synthesis to be more sustainable than the patented routes. Application of this green solvent was demonstrated for the first time for O– and N-arylation in SNAr reaction with solvent recovery with similar or superior yields compared to other green solvents. Moreover, broad opportunities for this green solvent in membrane science were identified, where the use of conventional, toxic polar aprotic solvents in large quantities is unavoidable. Important practical solvent properties and parameters such as dielectric constant, solubility parameters, solvent miscibility and NMR residual shifts have been determined to facilitate the uptake of methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate as a green solvent.

Towards cleaner PolarClean: efficient synthesis and extended applications of the polar aprotic solvent methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate

 Author affiliations

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https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC01958H?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

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Tetrahydrothiopyran-4-one as Five-Carbon Source for Scalable Synthesis of (±)-Tapentadol

 PROCESS, SYNTHESIS  Comments Off on Tetrahydrothiopyran-4-one as Five-Carbon Source for Scalable Synthesis of (±)-Tapentadol
Jul 122019
 

Abstract Image

Tetrahydrothiopyran-4-one as Five-Carbon Source for Scalable Synthesis of (±)-Tapentadol

 Ramagonolla Kranthikumar

  • Prathama S. Mainkar
  • Genji Sukumar
  • Rambabu Chegondi
  • Srivari Chandrasekhar*
Cite This:Org. Process Res. Dev.2019XXXXXXXXXX-XXX

Publication Date:June 26, 2019

https://doi.org/10.1021/acs.oprd.9b00121

The improved process for the synthesis of (±)-tapentadol, the FDA-approved analgesic drug, is achieved from tetrahydrothiopyran-4-one as the five-carbon source.

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MY AWARDS

 ANTHONY CRASTO, award  Comments Off on MY AWARDS
Jul 012019
 

 

anth1

My awards
http://amcrasto.weebly.com/awards.html


“100 Most Impactful Health care Leaders Global listing”, conferred at Taj lands end, Mumbai, India on 14 Feb 2017 by World Health Wellness congress and awards

“Best Worlddrugtracker “ Award for lifetime acheivement in Pharma… 7 th July 2017 , The venue…Taj land ends, Bandra, Mumbai India

“Lifetime achievement award” WORLD HEALTH CONGRESS 2017 in Hyderabad, 22 aug 2017 at JNTUH KUKATPALLY. HYDERABAD, TELANGANA, INDIA,

” Lifetime Achievement Award”, at the The Middle East Healthcare Leadership Awards – 12th October, 2017 -The Address, Dubai Mall, Dubai…UAE……….Mohammed Bin Rashid Boulevard, Downtown Dubai – Dubai – United Arab Emirates

International award for Outstanding contribution in Pharma at World Health and wellness Congress award, 14th Feb, 2018, at Taj Lands ends, Bandra, Mumbai, India

Conferred very prestigious IDMA award for contribution to society in Pharma at INDIAN DRUGS ANNUAL DAY 2018 VMCC IITBombay Powai, Mumbai India 22 Feb 2018,I was Guest of honor at and was felicitated by president,Indian Drug manufacturers association (IDMA)

Award conferred The Golden Globe Tigers Awards 2018, for Excellence in Pharma, at kuala lumpur, Malaysia, 23 april 2018 at Pullman hotel.

Conferred prestigious individual national award at function for contribution to Pharma society from Times Network, National Awards for Marketing Excellence ( For Excellence in HEALTHCARE) | 5th July, 2018 | Taj Lands End, Mumbai INDIA

Conferred award for Excellence in Pharma by CMO ASIA Award 31st July – 1st August, 2018 | Le Méridien Singapore, Sentosa

Life time Achievement Award by Bioleagues at 4th World Summit on Pharmaceutics Drug Designs, Dubai, UAE. Sep 21-22, 2018 at Flora creek Dubai UAE

Conferred prestigious ABPnews award for “Outstanding contribution to Education Sector” at event ABP News Presents Healthcare Leadership Awards 26th November, 2018 at Taj Lands End, Mumbai India

Honoured to get Award by ETnow for Outstanding contribution to social service at ET Now Presents World Mental Health Congress Co – Hosted with World Health & Wellness Awards, 15th February, 2019. | Taj Lands End, Mumbai, India

Honoured to get prestigious “SPER Innovative Researcher Award” The award was given in the SPER 8th Annual International Conference & Exhibition [SPER 2019] at VYWS’S Inst of pharma education and Research, Wardha [Maharashtra] India on February 23, 2019

Life time Achievement award at BioLEAGUES Worldwide at the 5th International Conference on Pharmaceuticals, API & Mfg. with the theme Enabling Technologies for API, Formulation & Manufacturing Aston Priority Simatupang Hotel & Conference Center, Jakarta, Indonesia on March 15th, 2019.

Lifetime achievement award, Prisal, Bhopal MP, India 26 may 2019 National Pharma Conference organized by Prisal, Pharmaceutical Royal International Society on Pharmaceuticals: Bench to Bedside: Challenges, Recent Initiatives & Future Perspectives
venue, State level animal husbandry auditorium, Bhopal

​Honoured to be conferred LIFE TIME ACHIEVEMENT AWARD by LOQMAN AWARDS ( National & International Awards ) on 23rd June 2019 Hotel Saffron leaf, Dehradun, Uttarakhand ,

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