posted on 2018-02-11, 00:00authored byRichard 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.