4.8 Article

Ni-Catalyzed Reductive Cross-Coupling of Cyclopropylamines and Other Strained Ring NHP Esters with (Hetero)Aryl Halides

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ORGANIC LETTERS
卷 24, 期 45, 页码 8441-8446

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.2c03570

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  1. NSERC
  2. Canada Foundation for Innovation [35261, 19119]
  3. Ontario Research Fund
  4. Alfred P. Sloan Foundation
  5. University of Toronto

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A nickel-catalyzed reductive cross-coupling reaction has been developed for the synthesis of 1-arylcyclopropylamines. The method is efficient, fast, and tolerant of different functional groups.
A nickel-catalyzed reductive cross-coupling of cyclopropylamine NHP esters with (hetero)aryl halides is reported. This efficient protocol provides direct access to 1-arylcyclopropylamines, a bioisosteric motif commonly used in small molecule drug discovery. The reaction proceeds rapidly (<2 h) with excellent functional group tolerance and without requiring heat-or air sensitive reagents. The method can also be extended to the arylation of four-membered strained rings. The NHP esters are easily obtained from the corresponding commercially available carboxylic acids in one step with high yields and no column chromatography.

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