4.8 Article

A General Method for Palladium-Catalyzed Direct Carbonylation of Indole with Alcohol and Phenol

Journal

ORGANIC LETTERS
Volume 14, Issue 16, Pages 4130-4133

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol3017726

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Funding

  1. Chinese Academy of Sciences
  2. National Natural Science Foundation of China [21002106, 21133011]

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A novel strategy involving a first oxidative iodination and subsequent Pd-0-catalyzed carbonylation to yield indole-3-carboxylate has been developed. It showed perfect generality to indole, alcohol, and phenol. The current methodology could also be conveniently applied to the synthesis of biologically active tropisetron from simple indole and tropine.

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