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Molecules 2004, 9(6), 405-426; doi:10.3390/90600405
Article

Synthesis of Chiral Building Blocks for Use in Drug Discovery

1, 1, 1, 1, 1, 1, 1, 1, 1, 1, 1,* , 2 and 3
1 Mimotopes Pty Ltd. 11 Duerdin Street, Clayton, Victoria 3168, Australia 2 School of Chemistry, University of Melbourne, Victoria 3010, Australia 3 Chiron Corporation, 4560 Horton St, Emeryville, California 94608, USA
* Author to whom correspondence should be addressed.
Received: 2 March 2004 / Accepted: 12 March 2004 / Published: 31 May 2004
(This article belongs to the Special Issue RACI 2003 symposium)
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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.
Keywords: chiral drugs; chiral building blocks; chiral metal catalysts; asymmetric hydrogenation; asymmetric epoxidation; DuPHOS; Noyori catalyst; Jacobsen’s catalyst. chiral drugs; chiral building blocks; chiral metal catalysts; asymmetric hydrogenation; asymmetric epoxidation; DuPHOS; Noyori catalyst; Jacobsen’s catalyst.
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Marino, S.T.; Stachurska-Buczek, D.; Huggins, D.A.; Krywult, B.M.; Sheehan, C.S.; Nguyen, T.; Choi, N.; Parsons, J.G.; Griffiths, P.G.; James, I.W.; Bray, A.M.; White, J.M.; Boyce, R.S. Synthesis of Chiral Building Blocks for Use in Drug Discovery. Molecules 2004, 9, 405-426.

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