An Effective And General Method For The Highly Regioselective Synthesis Of 1-phenylpyrazoles From β-enaminoketoesters, Tandem Blaise-acylation Adducts

摘要

An effective and general route for the regioselective synthesis of 1 -phenylpyrazoles has been developed from β-enaminoketoesters prepared by tandem Blaise-acylation. This method is applicable to a very broad range of substrates, generating a diverse set of 3-aryl-5-alkyl, 3-alkyl-5-aryl, 3,5-diaryl, and 3,5-dialkyl substituted pyrazoles regioselectively. The dichotomous regioselective synthesis of isotopically discriminated 3-CD_3-5-CH_3 and 3-CH_3-5-CD_3 substituted pyrazoles showcases the power of this protocol.