4.8 Article

Palladium-catalyzed difluoromethylthiolation of heteroaryl bromides, iodides, triflates and aryl iodides

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CHEMICAL SCIENCE
卷 7, 期 6, 页码 3757-3762

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c6sc00082g

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资金

  1. National Basic Research Program of China [2012CB821600]
  2. National Natural Science Foundation of China [21372247, 21572258, 21421002]
  3. SIOC

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A palladium-catalyzed difluoromethylthiolation of heteroaryl halides and triflates under mild conditions was described. A vast range of heteroaryl halides such as pyridyl, quinolinyl, benzothiazolyl, thiophenyl, carbazolyl and pyazolyl halides could be difluoromethylthiolated efficiently, thus providing medicinal chemists with new tools for their search of new lead compounds for drug discovery. Likewise, aryl iodides were difluoromethylthiolated in high yields under a modified reaction condition.

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