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

Sep 112019

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

Yuanyuan Zhou, Xianxiao Chen, Xiangxiang Ling and Weidong Rao

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

EP Patent Validation Service

PATENTS, Uncategorized Comments Off

Sep 062019

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%

Sandeep Mishra

Director at De Science Infoware Pvt Ltd

linkedin.com/in/sandeep-mishra-35b215b

scienceinfoware@gmail.com

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

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

Uncategorized Comments Off

Sep 042019

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

Felipe de Salas, Pablo Aza, Joan F. Francesc Gilabert, Gerard Santiago, Sibel Kiliç, Mehmet Emre Şener, Jesper Vind, Victor Guallar, Angel T. Martínez and Susana Camarero

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

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

green chemistry Comments Off

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 S_NAr 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

Levente Cseri*^a and Gyorgy Szekely*^a^b

Author affiliations

*Corresponding authors

^aSchool of Chemical Engineering and Analytical Science, University of Manchester, The Mill, Sackville Street, Manchester, UK
E-mail: levente.cseri@manchester.ac.uk, gyorgy.szekely@manchester.ac.uk
Tel: +44 (0)1613062662

^bAdvanced Membranes & Porous Materials Center, Physical Science Engineering Division (PSE), King Abdullah University of Science and Technology (KAUST), Thuwal 23955-6900, Saudi Arabia
E-mail: gyorgy.szekely@kaust.edu.sa
Tel: +966128082769

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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

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

PROCESS, SYNTHESIS Comments Off

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

Jul 012019

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 ,

Triple copper catalysis for the synthesis of vinyl triazoles

green chemistry, organic chemistry Comments Off

Jul 012019

Triple copper catalysis for the synthesis of vinyl triazoles

Green Chem., 2019, Advance Article
DOI: 10.1039/C9GC01066A, Communication

Lucas L. Baldassari, Eduardo A. Cechinatto, Angélica V. Moro
Herein, we report our studies on the synthesis of vinyl 1,2,3-triazoles through a one-pot sequence, enabled by the same copper catalyst, of three different reactions: hydroboration involving an alkyne, azidation for a vinyl boronate and azide–alkyne cycloaddition.
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

Triple copper catalysis for the synthesis of vinyl triazoles

Lucas L. Baldassari,^a Eduardo A. Cechinatto^a and Angélica V. Moro*^a

Author affiliations

*Corresponding authors

^aInstitute of Chemistry, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves 9500, Porto Alegre, Brazil
E-mail:angelica.venturini@ufrgs.br
Fax: +5551 3308 6259
Tel: +55 51 3308 9637

Abstract

Herein, we report our studies on the synthesis of vinyl 1,2,3-triazoles through a one-pot sequence, enabled by the same copper catalyst, of three different reactions: hydroboration involving an alkyne, azidation for a vinyl boronate and azide–alkyne cycloaddition.

https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC01066A?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

///////copper catalysis, vinyl triazoles

Pharmaceutical Royal International society (PRISAL), 1st Pharma conference, Bhopal, India 26 may 2019

ANTHONY CRASTO, CONFERENCE Comments Off

Apr 272019

Venue at State Animal Husbandry Training Institute , Bhopal, MP, India

We are delighted to have Dr.Anthony Melvin Crasto
Principal Scientist Glenmark Pharma as a “Guest of Honor ” at the 1st Pharma Conference on Pharmaceuticals -bench to bedside : challenges,recent initiatives and Future advancements in the Month of May 26th 2019. It will be a huge privilege to have you with us at this national conference.
#PRISAL

It is a Great honour indeed to be at Pharmaceutical Royal International society (PRISAL)
Thanks to Dr Priti Tagde for the honour and an opportunity to visit great city Bhopal MP, India for
1st Pharma Conference on Pharmaceuticals -bench to bedside : challenges,recent initiatives and Future advancements May 26th 2019. Bhopal, Mp, India

link https://www.facebook.com/Pharmaceutical-Royal-International-Society-2323710884572948/

www.prisalpharma.org

Pharmaceutical Royal International Society

DR PRITI TAGDE

+919098598114

💯 most impactful Healthcare Global leaders
Pharma Ratan Awardee
Outstanding Achievement Award

Associate Professor at Bhabha University

others……

Dr. Ranjit Barshikar , QbD international and Quality expert United Nations

Dr.Rupali Tasgaonkar
Principal Yadavrao Tasgaonkar Institute of Pharmacy

Mr. Sacheen Gandhi Co Founder FHER

Dr.Sidharth Mehan an Associate Professor ISF College of Pharmacy Moga Punjab

Dr.Narendra Joshi Senior Director Laxai Life Sciences

Dr.Murlidhar Ingle Director Adroit Pharma Pvt.Ltd

BHOPAL, MP, INDIA

Bada Talaab

Taj-ul-Masajid

Image result for bhopal

Raja Bhoj International Airport

Taj-ul-Masajid Aerial Photo

Train installation from Bhopal upper lake

FOOD IN BHOPAL

1. Jamal Bhai Tea Shop

Jamal Bhai Tea Shop

Source

Suleimani Chai is a special variety of tea that offers a fine balance of flavors, with a hint of sugar and salt. Served with a generous dollop of cream, it is sure to intrigue your taste buds and open your senses to a new day. This type of tea is offered in several parts of India, but the variety served in Bhopal is truly unique. And no better place to enjoy this tea, than Jamal Bhai Tea Shop at Itawar Chowk in Old Bhopal. You will know you have reached the right place when you see a large crowd of people sipping tea. The tea is served from a large samovar (something similar to a boiler used in the south). This slightly unusual and salty tea is certain to leave you mesmerized and wanting more.

2. Paya Soup in Chatori Gali

Paya Soup in Chatori Gali

Source

Chatori Gali is to Bhopal what Chandni Chowk is to Delhi, or Mohammed Ali Road is to Mumbai. If you happen to come to this food heaven, you simply cannot miss the mutton Paya soup, lamb slow-boiled in a broth all day long and delicately spiced. Quite unlike the Paya soup found in other parts of the country, the Paya soup served here is quite thick (by use of corn or wheat flour) and is less oily as well. Come sundown, the deliciously thick soup is poured into bowls, and is garnished with lamb shreds, spices and chopped coriander. It serves as a great appetizer, before you embark on a memorable gastronomic adventure in this humble gali.

3. Poha Jalebi at Kalyan Singh’s Swaad Bhandar

Poha Jalebi at Kalyan Singh's Swaad Bhandar

Source

If you are in the mood for some vegetarian goodness, the first place you should head out to is Kalyan Singh’s Swad Bhandar. Located on the east side of the Jama Masjid, off Itwara Road, it is always crowded and noisy here. Fresh, hot, moist, light and spicy Bhopali Poha garnished with a generous helping of crispy sev and served with some oh-so-yummy jalebis, it is sure to teleport you to food heaven. Poha Jalebi is the most famous breakfast that can be found all over M.P., but the best is found in Indore. These same Indoris serve this delicacy in Bhopal, making it a sumptuous and memorable breakfast that is light, enjoyable, delicious and easy on the pocket. Wash it down with a piping hot cup of Suleimani chai, and you can face all the troubles of the day head on.

4. Cycle Soupwala and Sagar Gaire Snacks

Cycle Soupwala and Sagar Gaire Snacks

Source

Bhopal’s famous Cycle Soupwala, located in Number 10, is a real-life rags-to-riches story. The owner of this humble eatery, so named because he sells delicious soup on a bicycle, came to this city from Nepal. He started off by selling three types of soup: tomato, sweet corn and manchow on a bicycle, to satisfy the hunger pangs of students and office-goers alike. His soup stall set him on the path to success and today he owns a chain of eateries in Bhopal, that serve everything from cold coffee to sandwiches, dosas to chole kulche. Neither his soup nor his eateries are something you should miss if you are in Bhopal, and looking for some yummy food.

5. Bade ke Kebab at Jhili Miyaan

Bade ke Kebab at Jhili Miyaan

Source

After a hard day’s work, if you are looking for something to set your taste buds on fire, Jhili Miyaan is the place to be. Located at the beginning of the Chatori Galli, this tiny shop sells the most amazing melt-in-your-mouth kebabs. Bade ke Kebab are essentially beef kebabs, made from minced beef, marinated all day in a spice mix. The kebabs are then rolled by hand, fried on a hot pan and stuffed inside grilled buns. The entire dish is made-to-order and is always served steaming hot served with a mix of onions, chutneys and chilies. Juicy, succulent kebabs, served with hot buns and a spicy chutney, is sure to melt away all your troubles. You can eat to your stomach’s content but never to your heart’s content!

6. Bhopali Paan

Bhopali Paan

Source

Paan is the traditional Indian way to end a meal in style. It is loved and consumed all over the country, and each region adds its own unique touch to the paan. Bhopali paan is very famous all over the country, and when you are here, this is not something you must miss. It is a pastry made from betel nut, stuffed with chuna, kattha and supari, and a generous dollop of gulkand. Paan-making is considered an art in Bhopal, and is part of the local culture. It is usually consumed as a mouth freshener though people can be found chewing paan throughout the day.

7. Shahi Tukda in Koh-e-Fiza

Shahi Tukda in Koh-e-Fiza

Source

If all the spicy food is making you nauseous and you need a refresher, Shahi Tukda is what you should have. Indulgence that is easy on the pocket, Shahi Tukda is the perfect sweet treat for you. It is made of fried bread soaked in a decadent custard, and garnished with nuts and spices. Don’t worry if things turn too sweet, that’s how it is meant to be in Bhopal. Koh-e-Fiza is the place to have this rich delicacy.

8. Kebabs at Jameel

Kebabs at Jameel

Source

After a hard day of shopping and doing touristy things in Old Bhopal, if you are on the hunt for some pet-pooja, head out to Jameel in Ibrahimpura. This is a busy lane in a busy area of the market housing a lot of bakeries, and the food is to die for! Rich succulent kebabs made of chicken or mutton, delicious egg curry and mutton stew ? all at a pocket-friendly price. Delicious food, fast service with affordable pricing, what else is it that you need?

9. Chaat at 6 Number Stop Hawkers Corner

Chaat_ 6 Number Stop Hawkers Corner

Source

If you are in the newer side of town and looking for some place to appease your taste buds, this one will not disappoint you. The Hawkers corner in 6 Number stop is sure to leave you drooling. Famous for all types of chaat like pani puri, dahi puri, bhel puri and chole tikki, and ice golas and faloodas, for those looking for something sweet, this is the most famous place to grab a quick bite. Special recommendation ? try the samosa kachori chaat. Tangy, tasty, spicy goodness that tickles your taste buds, leaving you wanting more.

10. Raju Tea Stall

Raju Tea Stall_Holdiify

Source

Also known as Fareed Bhai’s tea stall, it is hard to come across a Bhopali who has never had tea from this iconic tea stall, which is a landmark in itself. Situated in Old Bhopal near the Peer Gate area, it is the best location to have a cuppa with friends. Enjoy a steaming hot cup of Nawabi tea, which was a favorite of the royals and is famous among the locals, have some piping hot snacks, and just watch the city go by.

11. Barfi Rasmalai at Surendra Jain’s stall

Barfi Rasmalai _ Surendra Jain's stall_Holidify

Source

If you happen to be near the Jama Masjid, head over to the chowk adjacent to the masjid to taste something you have probably never tasted before ? barfi rasmalai drona. It is perhaps as whacky as it sounds, and is super-delicious. He takes a drona ( bowl made from dried leaves) , heaps up crushed ice, and then laps it up in a sweet, rich rabri, flavored syrup and rose water. Ice-cold, sweet and delicious, you would want to keep eating more of this wonderful street food. Have a bowlful as a palate refresher before you dig in through all those meat treats in Chatori Galli.

12. Manohar Dairy and Restaurant

Manohar Dairy and Restaurant_Holidify

Source

If you are in Bhopal, this is one place you absolutely must visit. A landmark in itself, Manohar Dairy and Restaurant has been standing tall since 1970 in Hamidia Road, and has been a witness to the growth of this buzzing city. As they keep adding in new restaurants and introducing a whole new array of dishes, the yesteryear charm is still intact. Two of their must-try dishes are the dahi puri and the chhole puri/kulche ? relished and recommended by generations of Bhopalis for years together.

13. Haji Lassiwala

Haji Lassiwala_Holidify

Source

A rich, decadent shake made from milk and cream, served with a generous helping of glassy, sugary, sweet noodles ? that is falooda for you. To make it even more irresistible, several flavoring syrups, dried fruits and nuts are added. It is a uniquely Indian dish and it is best had after a long post-dinner walk. And the best place to have it is Haji Lassiwala at Itwara Chowk in Old Bhopal. Locals say it is the world’s best falooda, and if a Bhopali says that, it might just be true!

14. Al Beik

This food joint has multiple franchises across Bhopal. An economical substitute to KFC, Al Beik serves mouth-watering Chicken Burgers, Nuggets, Chicken Strips making it a must-visit place for all chicken lovers.

Al Beik

Source

CREDIT

https://www.holidify.com/pages/bhopal-street-food-1506.html

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Basic Anion-Exchange Resin-Catalyzed Aldol Condensation of Aromatic Ketones with Aldehydes in Continuous Flow

organic chemistry, PROCESS Comments Off

Apr 262019

A general method for the aldol condensation of aromatic ketones with aldehydes was developed under continuous-flow conditions using a commercially available, strongly basic anion-exchange resin (A26) as catalyst. This procedure, in addition to exhibiting a wide substrate scope, promoted carbon–carbon bond formation under mild conditions using a quasi-stoichiometric ratio of starting reagents with good to excellent yields, thereby forming a limited amount of waste and allowing the process to be applied to sequential-flow systems. A proof of concept was developed in the first fully heterogeneously catalyzed two-step flow synthesis of donepezil, which is a blockbuster commercial anti-Alzheimer’s drug.

Basic Anion-Exchange Resin-Catalyzed Aldol Condensation of Aromatic Ketones with Aldehydes in Continuous Flow

Benjamin Laroche^†, Yuki Saito^†, Haruro Ishitani^‡, and Shu̅ Kobayashi*^†^‡

^†Department of Chemistry, School of Science, and ^‡Green & Sustainable Chemistry Social Cooperation Laboratory, Graduate School of Science, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.9b00048

*E-mail: shu_kobayashi@chem.s.u-tokyo.ac.jp.

https://pubs.acs.org/doi/10.1021/acs.oprd.9b00048

////////donepezil

Design, synthesis and antimicrobial activity of usnic acid derivatives

Uncategorized Comments Off

Feb 012019

Design, synthesis and antimicrobial activity of usnic acid derivatives

Victor Kartsev,^a Boris Lichitsky,^b Athina Geronikaki,*^c Anthi Petrou,^c Marija Smiljkovic,^d Marina Kostic,^d Oliver Radanovic^e and Marina Soković^d

Author affiliations

*Corresponding authors

^aInterBioscreen, Moscow, Russia

^bZelinsky Institute of Organic Chemistry, Leninsky Prospect, Moscow, Russia
E-mail: blich2006@mail.ru

^cSchool of Health, Department of Pharmacy, Aristotle University of Thessaloniki, Greece

^dMycological Laboratory, Department of Plant Physiology, Institute for Biological Research, Siniša Stanković, University of Belgrade, Bulevar Despota Stefana 142, Belgrade, Serbia

^eScientific Institute of Veterinary Medicine of Serbia, ul. Vojvode Toze 14, 11000 Belgrade, Serbia

Abstract

Usnic acid, a dibenzofuran, was originally isolated from lichens producing secondary metabolites, and is well known as an antibiotic, but is also endowed with several other interesting properties. Thus, the goal of this paper is the design of new usnic acid derivatives and evaluation of their antimicrobial activity. All newly synthesized compounds possess good antibacterial activity with MIC ranging from 1.02–50.93 × 10⁻² mmol mL⁻¹ and MBC from 2.05–70.57 × 10⁻² mmol mL⁻¹. The most sensitive bacterial species was Staphylococcus aureus, while Pseudomonas aeruginosa and Escherichia coli were the most resistant among the ATCC strains, and MRSA was the most resistant among all tested bacteria (ATCC and clinical isolates). Their antifungal activity was very strong (MIC = 0.35–7.53 × 10⁻² mmol mL⁻¹ and MFC = 0.70–15.05 × 10⁻² mmol mL⁻¹) – better than those of reference compounds and usnic acid itself. The most sensitive fungal species was Trichoderma viride, while Penicillium versicolor var. cyclopium appeared to be the most resistant. It should be mentioned that in general most of the compounds showed weaker antibacterial activity, but better antifungal properties than usnic acid itself. The results allow us to conclude that the title compounds are good lead compounds for novel more active antibacterial drugs. On the other hand, these compounds are very promising as antifungals.