Total synthesis of 26-hydroxy-epothilone B and related analogs via a macrolactonization based strategy

被引:45
作者
Nicolaou, KC
Finlay, MRV
Ninkovic, S
Sarabia, F
机构
[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
[3] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA
基金
美国国家卫生研究院;
关键词
D O I
10.1016/S0040-4020(98)00352-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The chemical synthesis of a series of 26-substituted epothilones B is described. Fully protected 26-hydroxydesoxyepothilone B (7), prepared via the macrolactonization strategy, served as a common precursor to the designed epothilones described. The synthesized compounds were members of a large epothilone library whose biological screening led to the identification of a number of highly potent antitumor agents. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:7127 / 7166
页数:40
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