Month: June 2014

(S)-Sitagliptin……….Synfacts by Thieme

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

New Drug Approvals

For description see at synfacts

Contributor: Philip Kocienski

Philip Kocienski, Professor of Organic Chemistry.

https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0033-1340505

Bao H, Bayeh L, Tambar UK * The University of Texas Southwestern Medical Center at Dallas, USA
Catalytic Enantioselective Allylic Amination of Olefins for the Synthesis of ent-Sitagliptin.

Synlett 2013;
24: 2459-2463

P. J. Kocienski
School of Chemistry
University of Leeds
Leeds LS2 9JT, UK
p.kocienski@chem.leeds.ac.uk
http://www.chem.leeds.ac.uk

Philip J. Kocienski was born in Troy, New York, in 1946. His love for organic chemsitry, amply stimulated by Alfred Viola whilst an undergraduate at Northeastern University, was further developed at Brown University, where he obtained his PhD degree in 1971 under Joseph Ciabattoni. Postdoctoral study with George Büchi at MIT and later with Basil Lythgoe at Leeds University, England, confirmed his interest in the synthesis of natural products. He was appointed Brotherton Research lecturer at Leeds in 1979 and Professor of Chemistry at Southampton University…

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Minisci reactions: Versatile CH-functionalizations for medicinal chemists

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

New Drug Approvals


View PDF Version
DOI: 10.1039/C1MD00134E (Review Article) Med. Chem. Commun.,2011, 2, 1135-1161

Minisci reactions: Versatile CH-functionalizations for medicinal chemists

Matthew A. J. Duncton†*
Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), Two Corporate Drive, South San Francisco, CA 94080, United States. E-mail: mattduncton@yahoo.com; Tel: +1 917-345-3183

Received 24th May 2011 , Accepted 3rd July 2011

First published on the web 22nd August 2011

http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e

http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e

http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e

http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e

http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e

http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e

The addition of a radical to a heteroaromatic base is commonly referred to as a Minsici reaction. Such reactions constitute a broad-set of selective CH-functionalization processes. This review describes some of the major applications of Minisci reactions and related processes to medicinal or biological chemistry, and highlights some potential developments within this area.

Introduction

The aim of this review is to summarize the use of Minisci reactions within medicinal chemistry…

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Memantine

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

New Drug Approvals

Memantine

1-amino-3,5-dimethyl adamantane

Memantina, Memantinum, Ebixa, 3,5-dimethyladamantan-1-amine, 1-Amino-3,5-dimethyladamantane, Memantin, CAS 19982-08-2, Memantinum [INN-Latin]
Molecular Formula: C12H21N   Molecular Weight: 179.30184
HCL SALT      41100-52-1

REVIEW BY ARK…..http://learnabout.arkpatentintelligence.com/drug-in-focus-memantine…… GREAT REVIEW BY


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Memantine is an orally active NMDA (N-methyl-D-aspartate) receptor antagonist which works by blocking the NMDA receptors in the brain. It blocks the excessive activity of glutamate, but still allows the normal activation of these receptors that occurs when the brain forms a memory. Therefore it improves the brain functioning in Alzheimer’s disease, and may also block the glutamate activity that could cause further damage to the brain cells.

Memantine hydrochloride is commercially available in the market in products…

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#realtimechemcarnival – New ChemDraw: What do I think?

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

The Organic Solution

A slightly different post in aid of the #realtimechemcarnival but hopefully useful to someone!

I currently use ChemDraw 13 Pro at work. This has very basic features and is really only useful for drawing out reaction schemes and checking molecular weights. At my previous workplace, I had ChemDrawUltra 2010. This had a lot of useful features like “convert name to structure” and NMR prediction, which were really useful tools, especially as I was writing my PhD thesis at the time.

Recently, I was given the chance to trial the new ChemBioDrawUltra 14.0. I expected this to be a better, flashier version of ChemDrawUltra 2010 and, indeed, it is. It has pretty much all the same useful tools as ChemDrawUltra 2010 but it also has some new features, which I have had fun playing around with.

What do I particularly like about this new version?

1) BioDraw tools – our group is very interdisciplinary. We currently…

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Highly efficient visible-light-driven photoelectro-catalytic selective aerobic oxidation of biomass alcohols to aldehydes

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

Green Chemistry International

Highly efficient visible-light-driven photoelectro-catalytic selective aerobic oxidation of biomass alcohols to aldehydes

Green Chem., 2014, Advance Article DOI: 10.1039/C4GC00454J,

http://pubs.rsc.org/en/Content/ArticleLanding/2014/GC/C4GC00454J?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

Paper Yajun Zhang, Guohua Zhao, Yanan Zhang, Xiaofeng Huang Highly efficient visible-light driven synergistic photoelectrocatalytic aerobic oxidation of biomass alcohols to aldehydes using Au/CeO2-TIO2 NT photocathodes under the mild conditions.

Department of Chemistry, Key Laboratory of Yangtze River Water Environment, Tongji University, Shanghai 200092, People’ s Republic of China
E-mail: g.zhao@mail.tongji.edu.cn;

A green and highly efficient visible-light-driven synergistic photoelectrochemical (PEC) catalysis system was systematically demonstrated for selective oxidation of biomass alcohols to the corresponding aldehydes in an O2 atmosphere under the mild conditions by employing the Au/CeO2–TiO2 NTs as photocathodes. Results showed that the conversion of benzyl alcohols was as high as 98% and the selectivity of benzaldehyde was >99% at the bias potential of −0.8 V under the visible light irradiation for 8 h…

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Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects

DR ANTHONY MELVIN CRASTO Ph.D Synthesis

New Drug Approvals

Graphical abstract: Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects

Graphical abstract: Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects

Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects

Dyanne L. Cruickshank, Yassir Younis, Nicholas M. Njuguna, Dennis S. B. Ongarora, Kelly Chibale and Mino R. Caira

CrystEngComm, 2014, 16, 5781 DOI:10.1039/C3CE41798K

http://pubs.rsc.org/en/Content/ArticleLanding/2014/CE/C3CE41798K?utm_medium=email&utm_campaign=pub-CE-vol-16-issue-26&utm_source=toc-alert#!divAbstract

3-(6-Methoxypyridin-3-yl)-5-(4-methylsulfonyl phenyl)-pyridin-2-amine (MMP) is a member of a novel class of orally active antimalarial drugs. This aminopyridine molecule has shown potent in vitro antiplasmodial activity and in vivo antimalarial activity in Plasmodium berghei-infected mice. The aqueous solubility of this molecule is, however, limited.

Thus investigations aimed at improving the physicochemical properties, including solubility, of MMP were accordingly conducted. Five salts of MMP were formed with co-former molecules saccharin, salicylic acid, fumaric acid, oxalic acid and suberic acid, but a cocrystal was obtained when the co-former adipic acid was employed.

All these new multi-component systems have been…

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