4.8 Article

C-N Cross-Couplings for Site-Selective Late-Stage Diversification via Aryl Sulfonium Salts

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 141, Issue 34, Pages 13346-13351

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jacs.9b07323

Keywords

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Funding

  1. MPI fur Kohlenforschung
  2. SNSF [P2EZP2_175112]
  3. Spanish Ministerio de Educacion, Cultura y Deporte [FPU15/03940, EST17/00459]
  4. Swiss National Science Foundation (SNF) [P2EZP2_175112] Funding Source: Swiss National Science Foundation (SNF)

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We report diverse C-N cross-coupling reactions of aryl thianthrenium salts that are formed site-selectively by direct C-H functionalization. The scope of N-nucleophiles ranges from primary and secondary alkyl and aryl amines to various N-containing heterocycles, and the overall transformation is applicable to late-stage functionalization of complex, drug-like small molecules.

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