Indian Pharma Market Needs Strong Regulatory Set-up: Kiran Mazumdar-Shaw

New Drug Approvals

Kiran Mazumdar-Shaw, MD, BIOCON

Indian Pharma Market Needs Strong Regulatory Set-up:   Kiran Mazumdar-Shaw, MD, BIOCON

Biocon is looking at gaining market share and improving its margins with a greater focus on its product mixes and organizational efficiencies. Biocon Chairman and Managing Director Kiran Mazumdar-Shaw tells Financial Express that the company has outpaced the market, despite various challenges and that the pharmaceutical market needs to have a more robust regulatory set-up. Edited excerpts:

READ ALL AT

http://kiranmazumdarshaw.blogspot.in/2013/07/indian-pharma-market-needs-strong.html

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Three-Bond Breaking of Cyclic Anhydrides: Easy Access to Polyfunctionalized Naphthalenes and Phenanthrenes

Three-Bond Breaking of Cyclic Anhydrides: Easy Access to Polyfunctionalized Naphthalenes and Phenanthrenes

Farnaz Jafarpour, Hamideh Hazrati, and Sorour Nouraldinmousa

School of Chemistry, College of Science, University of Tehran, 14155-6455 Tehran, Iran

Org. Lett., Article ASAP

Publication Date (Web): July 25, 2013 (Letter)

DOI: 10.1021/ol401318v

http://pubs.acs.org/doi/abs/10.1021/ol401318v

Benzannulation of phthalic anhydrides with alkynes to polyfunctionalized naphthalenes and phenanthrenes was confirmed to be straightforward using a palladium catalytic system. Sequential liberation of CO₂ and CO occurred via oxidative decomposition of anhydride. In the case of 1,8-naphthalenedicarboxylic anhydrides, both aryls were encompassed in the annulation reaction to afford acenaphthylenes.

Anthony crasto presentation of Biginelli reaction

Anthony crasto presentation of biginelli reaction from ANTHONY MELVIN CRASTO Ph.D

CSIR, INDIA-WO PATENT–synthesis of amprenavir and saquinavir

New Drug Approvals

amprenavir

saquinavir

A process for synthesis of syn azido epoxide and its use as intermediate in the synthesis of amprenavir and saquinavir
Published as ———WO-2013105118
Council of Scientific & Industrial Research

http://worldwide.espacenet.com:80/publicationDetails/biblio?CC=WO&NR=2013105118A1&KC=A1&FT=D&DB=EPODOC&locale=en_EP&date=20130718&rss=true

Inventors

Gadakh, Sunita, Khanderao; Rekula, Reddy, Santhosh; Sudalai, Arumugam
Publication date 18-JUL-2013

HIV protease inhibitor

Disclosed herein is a novel route of synthesis of syn azide epoxide of formu 5, which is used as a common intermdeiate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt- catalyzed hydrolyti kinetic resolution of racemic anti-(2SR, 3SR) – 3 -azido – 4 -phenyl – 1, 2- epoxybutane (azido-epoxide

IN2012DE82

10-JAN-2012 [priority]

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New clarity in the mechanism for lithium salt-free Wittig reactions

The Wittig reaction was first reported in 1954 and awarded the Nobel Prize in 1979.  Today, it is widely used for the preparation of alkenes by reaction of a carbonyl compound with a phosphonium ylide.  Despite its age and broad utility, differing mechanisms for the Wittig reaction still feature in the literature and textbooks.

Peter Byrne and Declan Gilheany at University College Dublin have written a substantial review of this transformation, which provides definitive evidence regarding the mechanism of lithium salt-free Wittig reactions of phosphonium ylides.

Phosphonium ylides can be represented in either ylide (1a) or ylene (1b) form and they are classified according to their substitution at the α-carbon.  The P–C­ bond of a phosphonium ylide is heavily polarised towards carbon and so ‘R’ groups that offer a greater degree of conjugative stabilisation increase the overall stabilisation of the ylide. Additionally, the nature of the ‘R’ group influences the selectivity for formation of Z or E alkenes.

The mechanism that features in many undergraduate textbooks involves the attack of the carbonyl carbon by the nucleophilic ylide α-carbon to form a betaine intermediate (7), which undergoes ring closure to form an oxaphosphetane (OPA) (8) and subsequently decomposes to form the product alkene (9) and a phosphine oxide (10) by-product.

Byrne and Gilheany present a body of evidence that disputes this mechanistic pathway and instead supports an irreversible [2 + 2] cycloaddition between the ylide and carbonyl compound to directly form the OPA (8).  The OPA then decomposes in a stereospecific manner, meaning that the stereochemistry of the alkene product is determined by the shape of the transition state for the [2 + 2] cycloaddition, and hence the structure of the OPA.  The E-selectivity commonly observed in the case of semi-stabilised and stabilised ylides is explained by a kinetic preference for the formation of trans-OPA, which decomposes to form the E-alkene.

This clarification of the mechanism for the lithium salt-free Wittig reaction will likely feature in future editions of undergraduate textbooks and will encourage many chemistry lecturers to update their course notes before the start of the new academic year.

For more, read this HOT Chem Soc Rev Review Article in full:

The Modern Interpretation of the Wittig Reaction Mechanism
Peter A. Byrne and Declan G. Gilheany

Centre for Synthesis & Chemical Biology, University College Dublin, Dublin 4, Ireland
E-mail: declan.gilheany@ucd.ie ;
Tel: +353-1-716-2308

Chem. Soc. Rev., 2013, Advance Article
DOI: 10.1039/C3CS60105F

Alice Williamson is a guest web-writer for Chem Soc Rev.  She is currently a postdoc for the OSDDMalaria Project in Dr. Matthew H Todd’s group at the University of Sydney.

http://sydney.edu.au/science/chemistry/aboutus/postdocs/williamson.html

How to Determine Boiling Points on the Microscale

Chemtips

How do you tell when a liquid boils, if you only have 10 μL?

This isn’t a subject I think about often, largely because I assumed the analysis would require complex equipment and most of an afternoon. Flipping through “Microscale Techniques for the Organic Laboratory” last week [1], I found an elegant work-around. All that’s needed is a standard melting point apparatus, a melting point tube, and a small bit of glass.  The limit of detection seems to be around 5 μL, though I tested the setup at about twice that.

The trick is to drop a tiny, inverted tube into the melting point tube, before adding the liquid of interest. The trapped pocket of air acts as a micro boiling stone, and as the liquid boils a steady stream of bubbles is evolved. The boiling point is thus the temperature at which sustained bubble…

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A Survey of Promising Late-Stage Diabetes Drugs

New Drug Approvals

 

THIS IS DEC2012 COMPILATION. READER MAY ENCOUNTER AN APPROVED OR DROPPED ENTRY

A variety of new drugs are in development for the treatment of type 1 or type 2 diabetes. In addition to new dipeptidyl peptidase-4 (DPP-IV) inhibitors, glucagon-like peptide (GLP) 1 analogs, basal insulin analogs, and new insulin formulations, there are also unique dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist, G-protein-coupled receptor (GPR) 40 agonist, sodium dependent glucose transporter 2 (SGLT2) inhibitor, and several other unique agents now in development.

A list of 25 drug candidates has been compiled for which diabetes is at least one proposed or approved indication, and for which one indication has reached Phase III or Registration phases. Each entry includes the name of the drug candidate, the sponsor, and, where applicable, chemical structures, collaboration partners; method of action; indication (by market, where applicable); and phase of trial. Some products are still in clinical…

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Naturalproductman's Blog

Stephen Martin and co-workers have reported in JACS on a synthesis of citirnadin A.

JACS paper

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HPV virus ‘linked to third of throat cancer cases’

Atasteofcreole's Blog

http://www.bbc.co.uk/news/health-23374920

One third of people diagnosed with throat cancer are infected with a form of the HPV virus, a study suggests.

HPV (human papillomavirus) is the major cause of cervical cancer, and the virus is known to spread through genital or oral contact.

Actor Michael Douglas is reported to have spoken about the link after his own diagnosis with throat cancer.

Experts said this study in the Journal of Clinical Oncology, which quantifies the link, showed “striking” results.

There are more than 100 types of HPV. Most people will be infected with HPV at some point, but in most the immune system will offer protection.

There are two HPV strains which are most likely to cause cancer – HPV-16 and HPV-18.

HPV-16 is thought to be responsible for around 60% of cervical cancers, 80% of cancers in the anus and 60% of oral cancers.

Around 1,500 people…

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Recent Progress in the Synthesis of Tamiflu

New Drug Approvals

ABOVE PICTURE-The synthetic route to tamiflu reported by M. Shibasaki starting from 1,4-cyclohexadiene. See JACS 2006, 128, 6312-6313

SEE  CHINESE ARTICLE ON  Recent Progress in the Synthesis of Tamiflu Zhang Tiancai, Lu Hui, Zhang Fu-Min, Cheng Jun, Liu Tianyang 2013, 33 (06), pp 1235-1243 Publication Date: 25 June 2013 (Reviews) DOI:10.6023/cjoc201303044

Abstract  Tamiflu, one of the most common orally drugs for the treatment and prevention of influenza, has attracted extensive interests of synthetic chemists all over the world.Concise, efficient, and scalable synthetic approaches toward this molecule have been a very active field in recent years, and many diverse synthetic routes have been developed to date.In this review, representative synthetic routes employing chiral starting material or catalytic asymmetric reactions are briefly summarized.
Fund:Project supported by the National Natural Science Foundation of China (Nos.20972059, 21290180), the Program for Changjiang Scholars and Innovative Research Team in…

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