4.8 Article

Palladium-catalyzed coupling of functionalized primary and secondary amines with aryl and heteroaryl halides: two ligands suffice in most cases

期刊

CHEMICAL SCIENCE
卷 2, 期 1, 页码 57-68

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c0sc00330a

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资金

  1. Amgen
  2. National Institutes of Health [GM-58160]
  3. Boehringer Ingelheim
  4. American Chemical Society
  5. National Science Foundation [CHE 9808061, DBI 9729592]
  6. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R37GM046059, R01GM058160] Funding Source: NIH RePORTER

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We report our studies on the use of two catalyst systems, based on the ligands BrettPhos and RuPhos, which provide the widest scope for Pd-catalyzed C-N cross-coupling reactions to date. Often low catalyst loadings and short reaction times can be used with functionalized aryl and heteroaryl coupling partners. The reactions are highly robust and can be set up and performed without the use of a glovebox. These catalysts should find wide application in the synthesis of complex molecules including pharmaceuticals, natural products and functional materials.

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