Hydrochloric Acid → (2S,4S)-4-Fluoropyrrolidine-2-carboxamide

Participants

Reaction Conditions

Reaction Steps

A mixture of (2S,4S)-2-carbamoyl-4-fluoro-pyrrolidine-1-carboxylic acid tert-butyl ester (1.0 g), conc. HCl (0.6 ml) and 1-butanol (10 ml) was heated for 48 h at 50° C. The RM was evaporated and partitioned DCM and aqueous NaHCO3, the DCM layers were dried over Na2SO4 and evaporated. A solution of 7 M ammonia in methanol (10 ml) was added to the residue and the mixture was stood for 60 h at it in a sealed vessel. Evaporation and trituration with EtOH gave the title compound as a white solid.

Provenance & Evidence