Formic Acid → HCID 10381826, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 188 mg (18 mmol) of acetic anhydride and 107 mg (23 mmol) of formic acid is prepared at 0° C., thereafter, heated to 60° C. for 2 hours. After cooling to RT, the mixture is diluted with 1 ml of tetrahydrofurane and a solution of 213 mg (7 mmol) of (R)-3-amino-1-[4-(3-fluoro-benzyloxy)-phenyl]-pyrrolidin-2-one in 2 ml of dichloromethane, beforehand prepared from the corresponding hydrochloride by treatment with triethylamine, is added. After the addition a white suspension is formed which is stirred at RT for 1 hour. For the working-up, the reaction mixture is treated with dichloromethane and water, then, the organic layer is separated, dried over sodium sulfate and evaporated. There are obtained 215 mg (92% of theory) of (R)-N-{1-[4-(3-Fluoro-benzyloxy)-phenyl]-2-oxo-pyrrolidin-3-yl}-formamide as a white solid; MS: m/e=329 (M+H)+.

Provenance & Evidence