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通过钯催化的烯烃双官能化反应合成并初步研究了 3-取代吲哚。

Synthesis and preliminary biological studies of 3-substituted indoles accessed by a palladium-catalyzed enantioselective alkene difunctionalization reaction.

机构信息

Department of Chemistry, University of Utah, 315 South 1400 East, Salt Lake City, Utah 84112, USA.

出版信息

J Am Chem Soc. 2010 Jun 16;132(23):7870-1. doi: 10.1021/ja103472a.

DOI:10.1021/ja103472a
PMID:20486685
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2896870/
Abstract

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.

摘要

一种独特的烯键双官能化反应，可以在生物相关的吲哚骨架周围快速构建分子复杂性。该反应的产率高达 87%，ee 值为 99:1，dr 值大于 20:1。对几种化合物的评估显示出对 MCF-7 细胞有良好的抗癌活性。

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