Short total synthesis of (+)-madindolines A and B

被引:40
作者
Hirose, T [1 ]
Sunazuka, T
Shirahata, T
Yamamoto, D
Harigaya, Y
Kuwajima, I
Omura, S
机构
[1] Kitasato Univ, Kitasato Inst, Minato Ku, Tokyo 1088642, Japan
[2] Kitasato Univ, Sch Pharmaceut Sci, Minato Ku, Tokyo 1088642, Japan
[3] Japan Sci & Technol Corp, JST, CREST, Minato Ku, Tokyo 1088642, Japan
关键词
D O I
10.1021/ol017058i
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A short and efficient total synthesis of (+)-madindolines A (1) and B (2), potent and selective inhibitors of interleukin 6, has been achieved. The synthesis features a key chelation-controlled 1,4-diastereoselective acylation to generate the quaternary carbon and an intramolecular acylation of allylsilane to build up the cyclopentene unit.
引用
收藏
页码:501 / 503
页数:3
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