(S)-Sitagliptin……….Synfacts by Thieme

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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Lipomycin synthesis

Naturalproductman's Blog

Reinhard Brückner and colleague at Albert-Ludwigs-Universität Freiburg have reported in ACIE on the synthesis of lipomycin.

ACIE paper

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Minisci reactions: Versatile CH-functionalizations for medicinal chemists

New Drug Approvals

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

Show CompoundsShow Chemical TermsShow Biomedical Terms

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

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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.

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Introduction

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

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Memantine

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?

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

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

New Drug Approvals

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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Polymorphs and co-crystals of haloprogin: an antifungal agent

New Drug Approvals

Haloprogin

Haloprogin is a topical antifungal agent. Its structure does not contain any of the functional groups typically exploited in hydrogen bond based co-crystal design. On the other hand, its 1-iodoalkyne moiety is nicely tailored to a crystal engineering strategy based on halogen bonding. Here we describe the formation of three polymorphs of haloprogin and of three co-crystals that this active pharmaceutical ingredient forms with both neutral and ionic co-crystal formers. The halogen bond plays a major role in all of the six structures and the interaction is thus confirmed to be a valuable tool which may complement the hydrogen bond when polymorphs and co-crystals of active pharmaceutical ingredients are pursued.

Graphical abstract: Polymorphs and co-crystals of haloprogin: an antifungal agent

http://pubs.rsc.org/en/Content/ArticleLanding/2014/CE/C4CE00367E?utm_medium=email&utm_campaign=pub-CE-vol-16-issue-26&utm_source=toc-alert#!divAbstract
Polymorphs and co-crystals of haloprogin: an antifungal agent

Michele Baldrighi,a Davide Bartesaghi,a Gabriella Cavallo,a Michele R. Chierotti,b Roberto Gobetto,b Pierangelo Metrangolo,*a Tullio Pilati,a Giuseppe Resnati*a and Giancarlo Terraneo*a

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Knowledge-based approaches to co-crystal design

New Drug Approvals

Knowledge-based approaches to co-crystal design – CrystEngComm (RSC Publishing) //

The use of knowledge-based methods has been intimately connected with the field of co-crystal design since the seminal papers of Etter and Desiraju in the 1990s. Here we explain and exemplify how rational co-crystal design has been carried out in the past using crystal structure knowledge as well as presenting emerging methodologies for knowledge-based co-former selection.

Peter A. Wood, Neil Feeder, Matthew Furlow, Peter T. A. Galek, Colin R. Groom and Elna Pidcock

CrystEngComm, 2014, 16, 5839 DOI:10.1039/C4CE00316K

http://pubs.rsc.org/en/Content/ArticleLanding/2014/CE/C4CE00316K?utm_medium=email&utm_campaign=pub-CE-vol-16-issue-26&utm_source=toc-alert#!divAbstract

Knowledge-based approaches to co-crystal design – CrystEngComm (RSC Publishing) //

Peter A. Wood,*^a  Neil Feeder,^a  Matthew Furlow,^a  Peter T. A. Galek,^a  Colin R. Groom^a and   Elna Pidcock^a  

*Corresponding authors

^aCambridge Crystallographic Data Centre, 12 Union Road, Cambridge, UK

E-mail: wood@ccdc.cam.ac.uk

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Exploring a parasitic tunnel boring machine

Lyra Nara Blog

Scanning electron micrograph of an adult whipworm roundworm parasite. Credit: Uta Rössler, Toby Starborg, Allison Bancroft and Richard Grencis, The University of Manchester.

Researchers have deduced essential biological and genetic information from the genome sequence of the whipworm, an intestinal parasitic worm that infects hundreds of millions of people in developing countries.

This information acts as the foundation for the development of new strategies and treatments against this debilitating parasite.

The whipworm is one of three types of soil-transmitted parasitic worms that collectively infect nearly two billion people. While infections often result in mild disease they may also lead to serious and long-term damage such as malnutrition, stunted growth and impaired learning ability. The full extent of worm-associated morbidity and the effect it has on socio-economic development in endemic countries is unknown.

This unusual parasite bores miniature tunnels through the lining of the large intestine where it may live for…

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