文献类型：期刊文献

英文题名：Economical Process for Preparation of the 19-nor A Ring of Paricalcitol from (-)-Shikimic Acid

作者：Zhou, Shengfeng[1];Zhu, Runyu[1];Hu, Jingwen[1];Zhang, Lixiong[1];Lu, Qian[1];Yu, Xinhong[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Engn Res Ctr Pharmaceut Proc Chem,Minist Educ, Shanghai Key Lab New Drug Design,State Key Lab Bi, Shanghai 200237, Peoples R China

年份：2019

卷号：23

期号：9

起止页码：1887

外文期刊名：ORGANIC PROCESS RESEARCH & DEVELOPMENT

收录：;EI(收录号：20193407346192);WOS:【SCI-EXPANDED(收录号:WOS:000487577100011)，CCR-EXPANDED(收录号:WOS:000487577100011)】；

基金：We gratefully acknowledge financial support from National Natural Science Foundation of China (21476078) and Science and Technology Commission of Shanghai Municipality (No. 12431900902).

语种：英文

外文关键词：Paricalcitol; 19-nor A ring; (-)-shikimic acid; Davis reagent

摘要：An economical and efficient means of preparing the 19-nor A ring, a key precursor of the vitamin D receptor (VDR) activator Paricalcitol, is here described. This process begins with commercially available (-)-shikimic acid and was easily scaled up to kilograms in a total yield over 17.8%. Davis oxidation was applied for the synthesis of the key precursor, a-hydroxyl carboxylic ester.