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Copper‐Catalyzed C−H Ethoxycarbonyldifluoromethylation of Indoles and Pyrroles
Author(s) -
Yan ShengYi,
Zhang ZhuoZhuo,
Liu YanHua,
Liao Gang,
Li PengXiang,
Shi BingFeng
Publication year - 2018
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.201800166
Subject(s) - chemistry , moiety , catalysis , combinatorial chemistry , copper , ligand (biochemistry) , phenanthroline , stereochemistry , functional group , medicinal chemistry , organic chemistry , receptor , biochemistry , polymer
An efficient copper‐catalyzed ethoxycarbonyldifluoromethylation of indoles and pyrroles with commercially available BrCF 2 CO 2 Et is reported. The developed protocol allows the site‐selective introduction of the CF 2 CO 2 Et moiety at the C2‐position of N‐heteroarenes with the assistance of a pyrimidyl group using CuI as the catalyst and 4,7‐diphenyl‐1,10‐phenanthroline as the ligand. This procedure is scalable and tolerates various important functional groups.