State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University , 38 Xueyuan Road, Beijing 100191, China.
Org Lett. 2017 Jul 7;19(13):3664-3667. doi: 10.1021/acs.orglett.7b01681. Epub 2017 Jun 22.
An efficient rhodium-catalyzed method for direct C-H functionalization at the C4 position of unprotected indoles has been developed. The utility of this method is demonstrated by the concise total syntheses of agroclavine and elymoclavine in a divergent manner. These syntheses feature a Pd-catalyzed asymmetric allylic alkylation reaction to assemble the triyclic indole moiety, and a ring-closing metathesis reaction to form the D ring.
已开发出一种高效的铑催化方法，可在未保护的吲哚的 C4 位置进行直接 C-H 功能化。该方法的实用性通过以发散方式简洁地总合成阿朴啡和麦角新碱得到证明。这些合成方法的特点是 Pd 催化的不对称烯丙基烷基化反应来组装三环吲哚部分，以及形成 D 环的闭环复分解反应。
