HMG-CoA还原酶抑制剂中间体合成新工艺  

New Process for a Pivotal Intermediate of the HMG-CoA Reductase Inhibitors

作　　者：王文金[1] 石炜[1] 徐勤耀[1] 杨琍苹[1] 

机构地区：[1]华东师范大学化学系,上海200062

出　　处：《有机化学》2008年第4期663-666,共4页Chinese Journal of Organic Chemistry

摘　　要：(3R,5S)-6-羟基-3,5-O,O-亚异丙基-二羟基己酸叔丁酯是制备HMG-CoA还原酶抑制剂的重要结构单元,提出了通过两次不对称催化氢化在温和的条件下方便高效高立体选择性合成(3R,5S)-6-羟基-3,5-O,O-亚异丙基-二羟基己酸叔丁酯的新工艺.该工艺8步总产率38%,de值99%.A new process was described for the preparation of t-butyl （3R,5S）-6-hydroxy-3,5-O,O-isopropylidenedioxyhexanoate, which is a key intermediate for a number of HMG-CoA reductase inhibitors. The intermediate was easily and efficiently obtained under mild reaction conditions via two enantioselective hydrogenation reactions with a high diastezeoselectivity of 99% de in an overall yield of 38% for the eight-step procedure.

关 键 词：对映选择性氢化 保护基 工业化 

分 类 号：TQ464.8[化学工程—制药化工]