Short total synthesis of (+)-madindolines A and B |
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| Authors: | Hirose Tomoyasu Sunazuka Toshiaki Shirahata Tatsuya Yamamoto Daisuke Harigaya Yoshihiro Kuwajima Isao Omura Satoshi |
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| Affiliation: | The Kitasato Institute and School of Pharmaceutical Sciences, Kitasato University, and CREST, The Japan Science and Technology Corporation (JST), Minato-ku, Tokyo 108-8642, Japan. |
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| Abstract: | ![]()
[reaction: see text] 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. |
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