Issue 36, 2015

Pd-catalyzed direct C2-acylation and C2,C7-diacylation of indoles: pyrimidine as an easily removable C–H directing group

Abstract

Pyrimidine is successfully used as an easily removable C(sp2)–H directing group for the synthesis of 2-acyl indoles and 2,7-diacyl indoles through direct C–H functionalization using a Pd-catalyst from 1-(pyrimidin-2-yl)-1H-indoles and aldehydes. Easy removal of the pyrimidine directing group using EtONa in DMSO provides C2-acyl indoles.

Graphical abstract: Pd-catalyzed direct C2-acylation and C2,C7-diacylation of indoles: pyrimidine as an easily removable C–H directing group

Supplementary files

Article information

Article type
Paper
Submitted
24 Nov 2014
Accepted
12 Mar 2015
First published
13 Mar 2015

RSC Adv., 2015,5, 28292-28298

Author version available

Pd-catalyzed direct C2-acylation and C2,C7-diacylation of indoles: pyrimidine as an easily removable C–H directing group

G. Kumar and G. Sekar, RSC Adv., 2015, 5, 28292 DOI: 10.1039/C4RA15162C

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