Pyrazole Formation using a 2 Step Reaction in Flow

We are pleased to share a new Flow Chemistry application note: #29: Pyrazole Formation using a 2 Step Reaction in Flow

Note #29 Tandem pyrazolePyrazoles are an important and well represented chemotype in drug discovery displaying wide-ranging biological actions that include analgesic, anti-inflammatory, antipyretic, tranquilizing,muscle relaxing,anticonvulsant, antidiabetic and antibacterial activities. The Pfizer Cox-2 inhibitor Celecoxib is a notable recent example.

This Application Note describes an efficient 2 step synthesis of a library of pyrazoles under continuous flow-through conditions developed by chemists at GalChimia. A starting acetophenone is first condensed with DMFDMA to form an intermediate enaminone followed by a second condensation with hydrazine to generate the desired pyrazoles.

The final condensation is performed using a Uniqsis glass static mixer chip.

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