Pyrazole synthesis via a cascade Sonogashira coupling/cyclization of N-propargyl sulfonylhydrazones

Abstract

An efficient approach for the preparation of pyrazoles via a Pd(II)/Cu(I)-catalyzed Sonogashira coupling/cyclization of N-propargyl sulfonylhydrazones has been established. In this study, we firstly report the strategic use of a Sonogashira reaction to construct pyrazole rings in a one step operation. With a broad range of functional group tolerance, bioactive 3-CF₃ pyrazoles can also be synthesized easily through this domino coupling/cyclization sequence.