4.8 Article

Synthesis and Preliminary Biological Studies of 3-Substituted Indoles Accessed by a Palladium-Catalyzed Enantioselective Alkene Difunctionalization Reaction

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 132, Issue 23, Pages 7870-+

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ja103472a

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Funding

  1. National Institutes of Health (NIGMS) [RO1GM3540, R01CA140296]
  2. DOD [W81XWH-09-1-0431]

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A unique alkene difunctionalization reaction that allows rapid construction of molecular complexity around the biologically relevant indole framework has been developed. The reaction proceeds with up to 87% yield, 99:1 er, and >20:1 dr. Evaluation of several of the compounds revealed promising anticancer activity against MCF-7 cells.

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