发明名称 |
Method for the preparation of (+)-calanolide A and analogues thereof |
摘要 |
A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (+/-)-8a. Separation and enzyme-mediated resolution of (+/-)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (+)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.
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申请公布号 |
US5859050(A) |
申请公布日期 |
1999.01.12 |
申请号 |
US19970926307 |
申请日期 |
1997.09.05 |
申请人 |
SARAWAK MEDICHEM PHARMACEUTICALS, INC. |
发明人 |
FLAVIN, MICHAEL T.;XU, ZE-QI;KHILEVICH, ALBERT;ZEMBOWER, DAVID;RIZZO, JOHN D.;LIN, LIN |
分类号 |
A61K45/06;C07D311/16;C07D493/04;C07D493/14;(IPC1-7):A61K31/35 |
主分类号 |
A61K45/06 |
代理机构 |
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代理人 |
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地址 |
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