Propiolic Acid → Cgp-47292

Participants

Reaction Steps

2,6-Difluorobenzyl azide (III) (7.0 g, 41.4 mmoles) is suspended in a H2O-tBuOH 1:1 mixture (120 ml), then propiolic acid (3.19 g, 45.6 mmoles), an ascorbic acid 1M solution (4.2 ml) and a CuSO4 0.3 M solution (1.4 ml) are added thereto. The reaction mixture is kept at 25° C. under stirring and is completed after 2 h. The mixture is left to cool at room temperature thereby precipitating the product. The solid is filtered off on a Buchner filter, washed with ethyl ether and dried under vacuum.

Provenance & Evidence