A facile route to paclitaxel C-10 carbamates

被引:7
作者
Ballatore, C [1 ]
Aspland, SE
Castillo, R
Desharnais, J
Eustaquio, T
Sun, SZ
Castellino, AJ
Smith, AB
机构
[1] Acidophil LLC, Suite 250,10835 Rd Cure, San Diego, CA 92121 USA
[2] Drexel Univ, Dept Chem, Philadelphia, PA 19104 USA
关键词
D O I
10.1016/j.bmcl.2005.03.072
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A general protocol for the synthesis of paclitaxel C-10 carbamates is described. The method entails MeI-mediated activation of 2'-O-TBS-7-O-TES-10-O-deacetyl-paclitaxel-10-O-carbonylimidazole prior to reaction with amines. This method is effective for the synthesis of paclitaxel C-10 derivatives, including bifunctional molecules. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2477 / 2480
页数:4
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