摘要

An efficient regioselective three-component synthesis of bipyrazoles4 by reaction of -aroylidineketene dithioacetals 1, Bestmann-Ohira reagent 2a and hydrazine hydrate 3 using KOH as a base in methanol medium was reported. Salient features of the present methodology are theregioselective construction of two pyrazoles unit contains four different heteroatoms (nitrogen, oxygen, sulfur and phosphorous) under mild reaction conditions with excellent yield in a single operation. In addition, unusual demethylation of methyl phosphorous ester group was observed. Based on the control experiments, plausible reaction mechanism was proposed.

  • 出版日期2017-3-23