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Heterocyclization of o-(arylethynyl)arylhydrazines as a new procedure for the synthesis of substituted 1H- and 2H-indazoles and indoles
Authors:Prikhodko  T A  Vasilevsky  S F
Institution:(1) Institute of Chemical Kinetics and Combustion, Siberian Branch of the Russian Academy of Sciences, 3 ul. Institutskaya, 630090 Novosibirsk, Russian Federation
Abstract:Procedures for the preparation of 3-substituted 1H- and 2H-indazoles and 2-substituted indoles were developed based on cross-coupling of o-iodoarylhydrazines with copper acetylenides in pyridine or dimethylformamide. An alternative procedure for the synthesis of 3-substituted 1H-indazoles involves cyclocondensation of (2-chloroaryl)acetylenes with hydrazine hydrate in butanol.
Keywords:indazoles  isoindazoles  indoles  cross-coupling  o-iodoarylhydrazines  o-chloroarylacetylenes  heterocyclization
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