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Cu-catalysed pyrazole synthesis in continuous flow†
Júlia Comas-Barceló,Daniel Blanco-Ania,Sebastiaan A. M. W. van den Broek,Pieter J. Nieuwland,Joseph P. A. Harrity,Floris P. J. T. Rutjes
Catalysis Science & Technology Pub Date : 02/08/2016 00:00:00 , DOI:10.1039/C5CY02247A
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.

Graphical abstract: Cu-catalysed pyrazole synthesis in continuous flow
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