摘要
(S)-(-)-环氧氯丙烷经氰化钠开环得到(S)-4-氯-3-羟基丁腈,用乙醇醇解得到(S)-4-氯-3-羟基丁酸乙酯,再经三甲硅烷基保护、氰化钠氰化、脱除保护基,得到阿伐他汀关键中间体(R)-(-)-4-氰基-3-羟基丁酸乙酯,总收率约57%。
Ethyl (R)-(-)-4-cyano-3-hydroxybutyrate was synthesized from (S)-(-)-epichlorohydrin by ring-opening with sodium cyanide to form (S)-4-chloro-3-hydroxybutyronitrile, which was subjected to alcoholysis, protection of hydroxyl group with hexamethyl disilazane, cyanidation and then deprotection with hydrochloric acid. The total yield was 57%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2009年第7期486-487,共2页
Chinese Journal of Pharmaceuticals