Ming-Liang Han, Wei Huang, Yu-Wen Liu, Min Liu, Hui Xu*, Hai Xiong*, and Hui-Xiong Dai*

Herein a palladium-catalyzed ligandpromoted asymmetric dearomatization of indoles via the decarbonylation of thioesters and the subsequent reductive Heck reaction is reported. This protocol provides a facile and efficient way to construct an aza-quaternary stereocenter at the C2 position of indolines. A variety of functional groups and substitutions could be well tolerated, affording the substituted indolines with high enantioselectivities.

https://dx.doi.org/10.1021/acs.orglett.0c03897