Synthesis 2015; 47(21): 3301-3308
DOI: 10.1055/s-0035-1560065
paper
© Georg Thieme Verlag Stuttgart · New York

N-Arylation of Sterically Hindered NH-Nucleophiles: Copper-Mediated­ Syntheses of Diverse N-Arylindole-2-carboxylates

Jinyong Lee
a   Medicinal Chemistry Research Center, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Daejeon 305-345, Republic of Korea   Email: indium@krict.re.kr
c   Graduate School of New Drug Discovery & Development Chungnam National University, Daejeon 305-764, Republic of Korea
,
Ji Hye Choi
a   Medicinal Chemistry Research Center, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Daejeon 305-345, Republic of Korea   Email: indium@krict.re.kr
b   Department of Chemistry, Hanyang University Seoul, 133-791, Republic of Korea
,
Seunghoon Shin
b   Department of Chemistry, Hanyang University Seoul, 133-791, Republic of Korea
,
Jung-Nyoung Heo
a   Medicinal Chemistry Research Center, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Daejeon 305-345, Republic of Korea   Email: indium@krict.re.kr
c   Graduate School of New Drug Discovery & Development Chungnam National University, Daejeon 305-764, Republic of Korea
,
Hwan Jung Lim*
a   Medicinal Chemistry Research Center, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Daejeon 305-345, Republic of Korea   Email: indium@krict.re.kr
d   Department of Medicinal and Pharmaceutical Chemistry, University of Science & Technology, 217 Gajeong-ro, Daejeon 305-350, Republic of Korea
› Author Affiliations
Further Information

Publication History

Received: 01 June 2015

Accepted after revision: 07 July 2015

Publication Date:
20 August 2015 (online)


Abstract

Indole-carboxylates are N-arylated with 2-bromopyridines using stoichiometric copper(II) oxide/potassium carbonate to give various N-(2-pyridyl)-substituted indole-2-carboxylates and with bromobenzenes using stoichiometric copper(I) iodide/N,N′-dimethylethylenediamine to give various N-(substituted phenyl)-substituted indole-2-carboxylates. These results expand the scope of metal-catalyzed N-ar­ylation using heterocyclic amines with steric bulk and weak nucleophil­icity.

Supporting Information