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
Mimotopes Pty Ltd. 11 Duerdin Street, Clayton, Victoria 3168, Australia.
Molecules. 2004 May 31;9(6):405-26. doi: 10.3390/90600405.
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.
在过去十年中，全球药品销售额显著增长，但更重要的是，单一异构体药物的销售额急剧增长。由于提高药物疗效的持续迫切需求，制药行业对手性中间体和研究试剂的需求不断增加。这反过来又影响到参与临床前发现工作的研究人员。除了传统的手性源和外消旋体拆分作为手性砌块的来源外，还开发了许多新的合成方法，包括各种各样的催化反应，这些方法有助于生产用于临床试验的复杂手性候选药物。最具雄心的技术是使用手性金属催化剂和相关化学方法从非手性起始原料合成纯手性化合物。本文介绍了利用不对称氢化和不对称环氧化从不手性原料合成手性砌块的实例。
