4.8 Article

Synthesis of Indolines by Palladium-Catalyzed Intermolecular Amination of Unactivated C(sp3)-H Bonds

Journal

ORGANIC LETTERS
Volume 21, Issue 16, Pages 6508-6512

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b02386

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Funding

  1. National Natural Science Foundation of China [216721626]
  2. Shanghai Science and Technology Commission [14DZ2261100]

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A new palladium-catalyzed C(sp(3))-H amination reaction has been developed. 1-(tert-Butyl)-2-iodobenzene and its derivatives undergo palladium-catalyzed C-H activation to form palladacycles. The palladacycles are aminated with diaziridinone to form indolines as the final products. The reaction represents a new method for the synthesis of 3,3-disubstituted indolines, which are essential structural motifs in many bioactive compounds and pharmaceutical targets.

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