Synthesis of a conformationally restricted analogue of paclitaxel

被引:12
作者
Barboni, L
Lambertucci, C
Ballini, R
Appendino, G
Bombardelli, E
机构
[1] Dipartimento Sci Chim, I-62032 Camerino, MC, Italy
[2] Dipartimento Sci & Tecnol Farmaco, I-10125 Turin, Italy
[3] Indena SPA, I-20141 Milan, Italy
关键词
D O I
10.1016/S0040-4039(98)01537-8
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A conformationally constrained analogue of the paclitaxel side-chain was synthesised in an enantioselective way from ethyl 1H-indene-2-carboxylate. Coupling with 7-triethylsilylbaccatin III and deprotection afforded 2',2 "-methylenepaclitaxel, a novel analogue of the natural product retaining anticancer activity. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:7177 / 7180
页数:4
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