Abstract

In the past decade there has been a significant growth in the sales of pharmaceutical drugs worldwide, but more importantly there has been a dramatic growth in the sales of single enantiomer drugs. The pharmaceutical industry has a rising demand for chiral intermediates and research reagents because of the continuing imperative to improve drug efficacy. This in turn impacts on researchers involved in preclinical discovery work. Besides traditional chiral pool and resolution of racemates as sources of chiral building blocks, many new synthetic methods including a great variety of catalytic reactions have been developed which facilitate the production of complex chiral drug candidates for clinical trials. The most ambitious technique is to synthesise homochiral compounds from non-chiral starting materials using chiral metal catalysts and related chemistry. Examples of the synthesis of chiral building blocks from achiral materials utilizing asymmetric hydrogenation and asymmetric epoxidation are presented.

Details

Title
Synthesis of Chiral Building Blocks for Use in Drug Discovery
Author
Marino, Sharon T; Stachurska-Buczek, Danuta; Huggins, Daniel A; Krywult, Beata M; Sheehan, Craig S; Nguyen, Thao; Choi, Neil; Parsons, Jack G; Griffiths, Peter G; James, Ian W; Bray, Andrew M; White, Jonathan M; Boyce, Rustum S
Pages
405-426
Publication year
2004
Publication date
2004
Publisher
MDPI AG
e-ISSN
14203049
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
1531107419
Copyright
Copyright MDPI AG 2004