Zhou Jianhui, Li Jian, Li Yazhou, Wu Chenglin, He Guoxue, Yang Qiaolan, Zhou Yu, Liu Hong
School of Pharmacy , Nanchang University , 461 Bayi Road , Nanchang 330006 , China.
State Key Laboratory of Drug Research and Key Laboratory of Receptor Research , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 555 Zu Chong Zhi Road , Shanghai 201203 , China.
Org Lett. 2018 Dec 7;20(23):7645-7649. doi: 10.1021/acs.orglett.8b03383. Epub 2018 Nov 20.
In the present study, a novel synthetic strategy to directly produce versatile 3-acylindoles through Rh(III)-catalyzed C-H activation and annulation cascade of N-phenylamidines with α-Cl ketones was developed, in which α-Cl ketones serve as unusual one-carbon (sp) synthons. This strategy features high regioselectivity, efficiency, wide substrate tolerance, and mild reaction conditions, which further underscore its synthetic utility in drug molecule synthesis.
在本研究中，开发了一种新颖的合成策略，通过铑（III）催化的N-苯基脒与α-氯代酮的C-H活化和环化串联反应直接制备多功能的3-酰基吲哚，其中α-氯代酮作为特殊的一碳（sp）合成子。该策略具有高区域选择性、高效性、广泛的底物耐受性和温和的反应条件，这进一步突出了其在药物分子合成中的实用价值。
