化学
苯并呋喃
吲哚试验
配体(生物化学)
组合化学
戒指(化学)
立体化学
有机化学
药物化学
受体
生物化学
作者
Chunchen Yuan,Changbo Jia,Wenlong Zhang,Yang’en You,Lei Zhu,Yongping Dong
标识
DOI:10.1021/acs.orglett.4c03173
摘要
A ligand-controlled method for the selective synthesis of indoles and benzofurans from secondary anilines has been discovered. A six-ring palladacycle intermediate may be involved in this process by olefins as a transient directing mediator to give indoles. The indole/benzofuran ratio can be easily tuned by the MPAA ligand. Various substituted secondary anilines were well-tolerated, affording the corresponding products in moderate to good yields. Indole-derived drugs such as JWH-081, BB-22, and ML-098 could be obtained using our new method to achieve their precursors. Preliminary mechanistic studies indicated that BQ is the key factor in avoiding the β-H elimination of insertion species.
科研通智能强力驱动
Strongly Powered by AbleSci AI