Cu-catalysed pyrazole synthesis in continuous flow

Abstract

The synthesis of 1,4-disubstituted pyrazoles via the cycloaddition reaction of sydnones and terminal alkynes has been achieved employing silica-supported copper catalysts. Furthermore, this methodology has been successfully implemented in continuous flow conditions using prepacked stainless steel cartridges containing the solid-supported copper promoter. Finally, we demonstrate that this synthetic procedure can be successfully scaled up to produce practically useful amounts of pyrazole products within 2-5 hours.