C-4 benzofuranylation of pyrazolones by a metal-free catalyzed indirect heteroarylation strategy

Abstract

A metal-free catalyzed indirect heteroarylation of pyrazolones with 2-(3-hydroxy-3,3-diarylprop-1-yn-1-yl) phenols has been developed, and a series of novel 4-benzofuranyl substituted pyrazolone derivatives were obtained in moderate to excellent yields (up to 90%). The process has the salient features of metal-free catalysis, operational simplicity, good substrate compatibility and mild reaction conditions. In particular, the integration of the pyrazolone skeleton and benzofuran scaffold into a single molecule is expected to be of potential interest for medicinal research. In addition, the yield and efficiency are basically maintained in the gram-scale experiment, which makes the practical application of the process more prominent.