A palladium-catalyzed intramolecular carbonylative annulation reaction for the synthesis of 4,5-fused tricyclic 2-quinolones
A palladium-catalyzed intramolecular carbonylative annulation reaction for the synthesis of 4,5-fused tricyclic 2-quinolones
复制标题
钯催化的分子内羰基环化反应合成 4,5-稠合三环 2-喹诺酮类药物
DOI：
10.1039/c6cc02600a
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发表时间：
2016
影响因子：
4.9
通讯作者：
Jia Yanxing
中科院分区：
文献类型：
--
作者：
Zhang Xiwu;Liu Haichao;Jia Yanxing
通过钯催化的炔键连接的N-取代邻碘苯胺的羰基成环反应，合成了4，5-稠合三环2-喹诺酮类化合物。该反应在温和的反应条件下顺利进行，并对各种官能团表现出优异的耐受性。它已成功应用于HIV整合酶抑制剂BI 224436的高效合成。
A concise and efficient synthetic route to 4,5-fused tricyclic 2-quinolones through the palladium-catalyzed carbonylative annulation of alkyne-tethered N-substituted o-iodoanilines has been developed. This reaction proceeds smoothly under mild reaction conditions and exhibits exceptional tolerance to a variety of functional groups. It has been successfully applied to the efficient synthesis of BI 224436, an HIV integrase inhibitor.