An Efficient Semi-Synthetic Method to Construct Docetaxel via Sterically Crowded Linear Side Chain Esterification  

作　　者：Xin Shen Jidong Yang Huaxing Zhan Hu Wang Shaohong Wu Zili Chen 

机构地区：[1]Shanghai Parling PharmaTech Co., Ltd., Suite 2, No. 868 Zhenchen Road, Baoshan District, Shanghai, 200444, China [2]Fujian South Pharmaceutical Co., Ltd., 98#, Dong-Xin Road, Xuefeng Town, Mingxi County, Fujian 365200, China [3]Department of Chemistry, Renmin University of China, Beijing 100872, China

出　　处：《Chinese Journal of Chemistry》2013年第1期31-36,共6页中国化学（英文版）

摘　　要：An efficient semi-synthetic method was developed to construct docetaxel 1 by using N,N-di-Boc protected lin- ear isoserine derivative 5 as the side chain source, in which, bulky protecting group on the nitrogen atom blocked C-2＇ position and prohibited unavoidable racemization in previous studies.An efficient semi-synthetic method was developed to construct docetaxel 1 by using N,N-di-Boc protected lin- ear isoserine derivative 5 as the side chain source, in which, bulky protecting group on the nitrogen atom blocked C-2＇ position and prohibited unavoidable racemization in previous studies.

关 键 词：DOCETAXEL SEMI-SYNTHESIS lO-deacetylbaccatin III ESTERIFICATION 

分 类 号：TQ463.5[化学工程—制药化工] O753.2[理学—晶体学]