Propiolic Acid → Cgp-47292

Participants

Reaction Steps

2,6-Difluorobenzyl azide (III) (3.5 g, 20.7 mmoles) is suspended in a H2O-tBuOH 1:1 mixture (80 ml), then propiolic acid (1.59 g, 22.8 mmoles), an ascorbic acid 1M solution (2.1 ml) and a CuSO4 0.3 M solution (0.7 ml) are added thereto. The reaction mixture is kept at 40° 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