New practical synthesis of indazoles via condensation of o-fluorobenzaldehydes and their O-methyloximes with hydrazine |
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Authors: | Lukin Kirill Hsu Margaret C Fernando Dilinie Leanna M Robert |
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Institution: | GPRD Process Research and Development, Abbott Laboratories, North Chicago, Illinois 60064, USA. kirill.lukin@abbott.com |
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Abstract: | The reaction of o-fluorobenzaldehydes and their O-methyloximes with hydrazine has been developed as a new practical synthesis of indazoles. Utilization of the methyloxime derivatives of benzaldehydes (in the form of the major E-isomers) in this condensation effectively eliminated a competitive Wolf-Kishner reduction to fluorotoluenes, which was observed in the direct preparations of indazoles from aldehydes. Reaction of Z-isomers of methyloximes with hydrazine resulted in the formation of 3-aminoindazoles via a benzonitrile intermediate. |
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