Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 76, Issue 11, Pages 4753-4758Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo200561f
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- CSIR, New Delhi
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An efficient method for regio- and chemoselective Friedel-Crafts acylation of indole using acyl chlorides in the presence of ZrCl4 has been discovered. It minimizes/eliminates common competing reactions that occur due to high and multiatom-nucleophilic character of indole. In this method, a wide range of aroyl, heteroaroyl alkenoyl, and alkanoyl chlorides undergo smooth acylation with various indoles without NH protection and afford 3-acylindoles in good to high yields.
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