4.8 Article

Construction of Atropisomeric 3-Arylindoles via Enantioselective Cacchi Reaction

Journal

ORGANIC LETTERS
Volume 23, Issue 15, Pages 5901-5905

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c02012

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Funding

  1. Fundamental Research Funds for the Central Universities [GK202103040, 2020CSLZ004]
  2. SNNU

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The de novo construction of axially chiral 3-arylindoles bearing a C(3)-C(aryl) chiral axis has been successfully achieved through a Pd-catalyzed enantioselective Cacchi reaction between aryl bromides and o-alkynylanilines. The reaction proceeds under mild conditions with high yields and excellent enantioselectivities.
The de novo construction of axially chiral 3-arylindoles bearing a C(3)-C(aryl) chiral axis has been realized by Pd-catalyzed enantioselective Cacchi reaction between aryl bromides and o-alkynylanilines. The reaction proceeded under mild conditions in high yields and excellent enantioselectivities.

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