4.7 Article

Cascade One-Pot Method To Synthesize Isoquinolin-1(2H)-ones with alpha-Bromo Ketones and Benzamides via Pd-catalyzed C-H Activation

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 83, Issue 4, Pages 2317-2323

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.7b03224

Keywords

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Funding

  1. National Science Foundation of China [21572117]
  2. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia medica, Chinese Academy of Medical Sciences, and Peking Union Medical College [GTZK201707]

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A cross-coupling strategy of palladium-catalyzed ortho-C-H bond activation and intramolecular addition of N-C annulation to synthesize isoquinolin-1(2H)-ones has been developed. A wide range of alpha-bromo ketones with different substituents proceeded smoothly in this reaction, and varieties of isoquinolin-1(2H)-one derivatives were obtained in moderate to good yields.

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