1286208-55-6

1257046-87-9

1286208-55-6

General procedure for the synthesis of R-1-acetyl-3-aminopyrrolidine hydrochloride from tert-butyl (R)-(1-acetylpyrrolidin-3-yl)carbamate: tert-butyl N-[(3R)-1-acetylpyrrolidin-3-yl]carbamate (Intermediate 14, 90 g, 0.39 mol) was slowly added to 1 L of HCl/MeOH solution at 0 °C. The reaction mixture was stirred at room temperature for 3 hours. After completion of the reaction, the mixture was concentrated and the residue was washed with ether to afford R-1-acetyl-3-aminopyrrolidine hydrochloride (55 g, 85% yield) as a white solid. The product was characterized by 1H NMR (300 MHz, MeOD): δ 2.12 (3H, m), 2.18-2.48 (2H, m), 3.56-3.79 (4H, m), 3.92-3.96 (1H, m). No mass ion peaks were observed; HPLC retention time tR = 2.78 min.