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/ol901208d | DOI Listing |
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