(1R,2S)-(–)-麻黄碱盐酸盐的合成

Synthesis of (1R,2S)-(–)-Ephedrine Hydrochloride

设计并实现了(1R,2S)-(–)-麻黄碱盐酸盐的一种不对称合成法,以2-溴-1-苯基-1-丙酮为起始原料,经(S)-α-苯乙胺胺化、分离、KBH4立体选择性还原、Leuckart反应及钯炭脱苄等制得目标物,总收率约25%。

A new synthesis of （1R,2S）- （-） -ephedrine hydrochloride was achieved, started from 2-bromo- 1-ph.enyl-1-propanone. The product was obtained by amination with （S）-α-methylbenzylamine, separation of the diastereoisomers, stereoselective reduction, Leuckart reaction and then debenzylation with an overall yield of about 25 %.