发明名称 |
Method for synthesizing epothilones and epothilone analogs |
摘要 |
A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.
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申请公布号 |
US2003187273(A1) |
申请公布日期 |
2003.10.02 |
申请号 |
US20030352340 |
申请日期 |
2003.01.27 |
申请人 |
OREGON STATE UNIVERSITY |
发明人 |
WHITE JAMES DAVID;CARTER RICH GARRETT;SUNDERMANN KURT FREDERICK |
分类号 |
C07D277/20;C07D417/06;(IPC1-7):C07D417/02 |
主分类号 |
C07D277/20 |
代理机构 |
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主权项 |
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地址 |
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