AUTHOR OF THIS BLOG

DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

IMPROVING CHEMICAL SYNTHESIS USING FLOW REACTORS.

 SYNTHESIS  Comments Off on IMPROVING CHEMICAL SYNTHESIS USING FLOW REACTORS.
Jan 242015
 
Expert Opin Drug Discov
Expert Opin Drug Discov 2007 Nov;2(11):1487-503
Charlotte                                                Prof Paul Watts

Owing to the competitive nature of the pharmaceutical industry, researchers involved in lead compound generation are under continued pressure to identify and develop promising programmes of research in order to secure intellectual property.

The potential of a compound for therapeutic development depends not only on structural complexity, but also on the identification of synthetic strategies that will enable the compound to be prepared on the desired scale.

One approach that is of present interest to the pharmaceutical industry is the use of continuous flow reactors, with the flexible nature of the technology being particularly attractive as it bridges the changes in scale required between the initial identification of a target compound and its subsequent production.

Based on these factors, a significant programme of research is presently underway into the development of flow reactors as tools for the synthetic chemist, with the transfer of many classes of reaction successfully reported to date.

This article focuses on the application of continuous flow methodology to drug discovery and the subsequent production of pharmaceuticals.

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Synthesis of Methoxyisopropyl (MIP)-Protected (R)-Mandelonitrile and Derivatives in a Flow Reactor

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Jan 042015
 

 

 

 

Cyanohydrins are synthetically versatile chiral building blocks in organic synthesis. They can be conveniently synthesized in enantiomerically pure form via chemoenzymatic hydrogen cyanide addition onto the corresponding aldehyde using hydroxynitrile lyase.

Recently, we reported that such transformations can be efficiently carried out in a continuous flow manner using microreactors. Since racemization of enantiopure cyanohydrins occurs readily under slightly basic conditions, they should be protected before the follow-up reactions, preferably under acidic conditions.

In this contribution, we demonstrate that the methoxyisopropyl protection of mandelonitrile can be conveniently optimized in an automated microscale continuous flow system and subsequently scaled up under the same conditions by applying a larger flow reactor.

 

Synthesis of Methoxyisopropyl (MIP)-Protected (R)-Mandelonitrile and Derivatives in a Flow Reactor

http://www.akademiai.com/content/9488206462627n38/?p=6ed413d7b9fb47fe9fe7e1262c37694f&pi=2

Journal of Flow Chemistry
Publisher Akadémiai Kiadó
ISSN 2062-249X (Print)
2063-0212 (Online)
Subject Flow Chemistry
Issue Volume 2, Number 4/December 2012
Pages 124-128
DOI 10.1556/JFC-D-12-00008

Radboud University

Authors
Mariëlle M.E. Delville, Jasper J.F. Gool, Ivo M. Wijk, Jan C.M. Hest, Floris P.J.T. Rutjes1 Email for f.rutjes@science.ru.nl  f.rutjes@science.ru.nl

1Institute for Molecules and Materials Radboud University Nijmegen Heyendaalseweg 135 6525 AJ Nijmegen the Netherlands

Floris P.J.T. Rutjes

Groepsfoto IMM 2014 klein-1

 

The IMM-office is located on the 3rd floor of the Huygens building, which is at walking distance (about 5 min.) from the railway station Nijmegen Heyendaal.

 

 

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