Regioselective synthesis of 2 H-indazoles using a mild, one-pot condensation-cadogan reductive cyclization
An operationally simple and efficient one-pot synthesis of 2H-indazoles from commercially available reagents is reported. Ortho-imino-nitrobenzene substrates, generated via condensation, undergo reductive cyclization promoted by tri-n-butylphosophine to afford substituted 2H-indazoles under mild reaction conditions. A variety of electronically diverse ortho-nitrobenzaldehydes and anilines were examined. To further extend the scope of the transformation, aliphatic amines were also employed to form N2-alkyl indazoles selectively under the optimized reaction conditions.
Genung, Nathan E.,Wei, Liuqing,Aspnes, Gary E.
p. 3114 - 3117
(2014/06/23)
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