New approach to paricalcitol synthesis  

作　　者：LI LiQi YUE LiRong XIE ZhiXiang LI Ying 

机构地区：[1]State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China

出　　处：《Chinese Science Bulletin》2012年第14期1616-1619,共4页

基　　金：supported by the National Natural Science Foundation of China (20802028 and 21072084)

摘　　要：Paricalcitol,an analog of vitamin D,is used as a drug for the prevention and treatment of secondary hyperparathyroidism.In this paper,a new strategy for the synthesis of paricalcitol is described.This approach includes three main improvements:one-pot regioselective ozonization cleavage of the side-chain and methylene at C-19,free-radical reduction removal of the OH group formed at C-19,and side-chain assembly using a Wittig reaction.These are all new strategies for the synthesis of 19-nor-vitamin D2 compounds.Paricalcitol, an analog of vitamin D, is used as a drug for the prevention and treatment of secondary hyperparathyroidism. In this paper, a new strategy for the synthesis of paricalcitol is described. This approach includes three main improvements： one-pot regioselective ozonization cleavage of the side-chain and methylene at C-19, free-radical reduction removal of the OH group formed at C-19, and side-chain assembly using a Wittig reaction. These are all new strategies for the synthesis of 19-nor-vitamin D2 compounds.

关 键 词：醇合成 维生素D2 清除自由基 反应选择性 甲状旁腺 继发性 亚甲基 化合物 

分 类 号：TQ466.4[化学工程—制药化工]