发明名称 |
AN ARYLATION METHOD FOR THE FUNCTIONALIZATION OF O-ALLYL ERYTHROMYCIN DERIVATIVES |
摘要 |
An efficient arylation technique for use in the synthesis of erythromycin derivatives, involving a modified Heck reaction which employs less than six mole percent of palladium catalyst and no phosphine is disclosed. With this modified Heck reaction, an O-alkenylaryl macrolide can be obtained in a much shorter reaction time than under conventional Heck reaction conditions. The modified Heck reaction can be utilized in a method for phosphine-free arylation of an O-allylic erythromycin derivative, in a method for preparing an O-alkenylaryl erythromycin A derivative, or in a method for preparing a 2', 4"-hydroxyl protected 6-O-alkenylaryl erythromycin A derivative.
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申请公布号 |
WO02096922(A1) |
申请公布日期 |
2002.12.05 |
申请号 |
WO2002US18348 |
申请日期 |
2002.05.21 |
申请人 |
ABBOTT LABORATORIES |
发明人 |
ZHANG, WEIJIANG;HSU, MARGARET, CHI-PING;HAIGHT, ANTHONY, R.;PETERSON, MATTHEW, JOHN;NARAYANAN, BIKSHANDARKOIL, A. |
分类号 |
A61K31/7048;A61P31/04;C07B61/00;C07H17/08;(IPC1-7):C07H17/08 |
主分类号 |
A61K31/7048 |
代理机构 |
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主权项 |
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地址 |
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