Zhang Xiwu, Liu Haichao, Jia Yanxing
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.
Chem Commun (Camb). 2016 Jun 8;52(49):7665-7. doi: 10.1039/c6cc02600a.
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.
通过钯催化的炔基连接的N-取代邻碘苯胺的羰基化环化反应，开发了一种简洁高效的合成4,5-稠合三环2-喹诺酮的路线。该反应在温和的反应条件下顺利进行，对各种官能团具有出色的耐受性。它已成功应用于HIV整合酶抑制剂BI 224436的高效合成。
