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Strategy To Prepare 3‑Bromo- and 3‑Chloropyrazoles

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journal contribution
posted on 2018-02-11, 00:00 authored by Richard J. Fox, Michael A. Schmidt, Martin D. Eastgate
A general strategy to prepare substituted 3-bromo- and 3-chloropyrazoles is described. The three-step method involves condensation of crotonates or β-chloro carboxylic acids with hydrazines, followed by halogenation and oxidation. Several condensation and oxidation protocols were developed to enable preparation of a wide variety of 3-halopyrazoles with good to excellent yields and regiocontrol.

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