发明名称 |
IMPROVED PROCESS FOR THE PREPARATION OF EZETIMIBE |
摘要 |
<p>The present invention relates to a cost effective and industrially advantageous process for the preparation of (3R,4S)-1-(4-fluorophenyl)-3-[3(S)-3-(4-fluorophenyl)-3-hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone, referred to here as Ezetimibe and represented by structural formula (I). The process comprises an multi-step reaction sequence that includes a chiral auxiliary-controlled condensation, a silyl-mediated cyclization, a palladium-catalyzed Negishi cross-coupling, and the enantioselective reduction of a ketone to a hydroxyl group.</p> |
申请公布号 |
EP1893570(A4) |
申请公布日期 |
2009.12.23 |
申请号 |
EP20060711373 |
申请日期 |
2006.02.17 |
申请人 |
SATYNARAYANA REDDY, MANNE;KISHORE KUMAR, MUPPA;SAHADEVA REDDY, MARAMREDDY |
发明人 |
SATYNARAYANA REDDY, MANNE;KISHORE KUMAR, MUPPA;SAHADEVA REDDY, MARAMREDDY |
分类号 |
C07D205/08 |
主分类号 |
C07D205/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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