Synthesis of fully substituted pyrazoles via regio- and chemoselective metalations.

Org Lett

Department Chemie & Biochemie, Ludwig-Maximilians-Universität, Butenandtstrasse 5-13, 81377 München, Germany.

Published: August 2009

The full functionalization of the pyrazole ring was achieved by successive regioselective metalations using TMPMgCl x LiCl and TMP(2)Mg x 2 LiCl. Trapping with various electrophiles led to trisubstituted pyrazoles. An application to the synthesis of the acaricide Tebufenpyrad is reported.

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http://dx.doi.org/10.1021/ol901208dDOI Listing

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