Synthesis of chiral building blocks for use in drug discovery.
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.
Marino
Sharon T
ST
Mimotopes Pty Ltd. 11 Duerdin Street, Clayton, Victoria 3168, Australia.
Stachurska-Buczek
Danuta
D
Huggins
Daniel A
DA
Krywult
Beata M
BM
Sheehan
Craig S
CS
Nguyen
Thao
T
Choi
Neil
N
Parsons
Jack G
JG
Griffiths
Peter G
PG
James
Ian W
IW
Bray
Andrew M
AM
White
Jonathan M
JM
Boyce
Rustum S
RS
D002384:Catalysis; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004852:Epoxy Compounds / Q000737:chemistry; D006865:Hydrogenation; D015394:Molecular Structure; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis / Q000737:chemistry; D013237:Stereoisomerism
D004852:Epoxy Compounds; D004364:Pharmaceutical Preparations