Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (04): 663-666. Previous Articles     Next Articles

Original Articles

HMG-CoA还原酶抑制剂中间体合成新工艺

王文金,石炜,徐勤耀,杨琍苹*   

  1. (华东师范大学化学系 上海 200062)
  • 收稿日期:2007-01-05 修回日期:2007-06-27 发布日期:2008-04-17
  • 通讯作者: 杨琍苹

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

WANG Wen-Jin,SHI Wei,XU Qin-Yao,YANG Li-Ping*   

  1. (Department of Chemistry, East China Normal University, Shanghai 200062)
  • Received:2007-01-05 Revised:2007-06-27 Published:2008-04-17
  • Contact: YANG Li-Ping

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 di-astezeoselectivity of 99% de in an overall yield of 38% for the eight-step procedure.

Key words: protecting group, enantioselective hydrogenation, industrialization