Pd-Catalyzed Asymmetric Dearomatization of Indoles via Decarbonylative Heck-Type Reaction of Thioesters

Authors:

Abstract
We report herein a palladium-catalyzed ligand-promoted asymmetric dearomatization of indoles via the decarbonylation of thioesters and the subsequent reductive Heck reaction. 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.
Funding Information
  • Ministry of Science and Technology of the People's Republic of China (2018ZX09711002-006)
  • Youth Innovation Promotion Association of the Chinese Academy of Sciences (2014229, 2018293)
  • Science, Technology and Innovation Commission of Shenzhen Municipality (KQJSCX20180328095517269)
  • Science and Technology Commission of Shanghai Municipality (17JC1405000, 18431907100, 19XD1424600)
  • National Natural Science Foundation of China (21772211)
  • Chinese Academy of Sciences (CASIMM0120163006)
  • State Key Laboratory of Natural and Biomimetic Drugs, Peking University
  • Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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