IMPROVED PROTECTION AND ESTERIFICATION OF A PRECURSOR OF THE TAXOTERE(R) AND TAXOL SIDE-CHAINS

被引:150
作者
COMMERCON, A
BEZARD, D
BERNARD, F
BOURZAT, JD
机构
[1] Rhône-Poulenc Rorer - Centre de Recherches de Vitry-Alfortville 13, 94403 Vitry-sur-Seine
关键词
D O I
10.1016/S0040-4039(00)79128-3
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
(4S,5R)-N-BOC-2,2-dimethyl-4-phenyl-5-oxazolidinecarboxylic acid 8 was prepared and efficiently esterified by conveniently protected baccatins 9a,b. Smooth deprotection in formic acid gave the N-deprotected intermediates of Taxotere(R) and taxol. This protocol did not generate any epimerization at C-2' and constitutes a pratical method to prepare Taxotere(R), taxol and analogs.
引用
收藏
页码:5185 / 5188
页数:4
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