3-N-Boc-aminopyrrolidine

99735-30-5

99724-19-3

General procedure for the synthesis of 3-(Boc-amino)pyrrolidine from 1-benzyl-3-(Boc-amino)pyrrolidine: 1-benzyl-3-(Boc-amino)pyrrolidine (15.75 g, 57.0 mmol) was dissolved in a solvent mixture of methanol and tetrahydrofuran (4:1, 114 ml) in a 500 ml reaction vessel. A catalytic amount of 10% palladium/carbon (Pd/C) was added to the solution. The reaction mixture was stirred and reacted for 12 hours under hydrogen atmosphere. Upon completion of the reaction, the palladium/carbon catalyst was removed by filtration through a diatomaceous earth pad and the filtrate was concentrated under reduced pressure to remove the solvent. The resulting residue was purified by silica gel column chromatography to afford 3-(Boc-amino)pyrrolidine (9.51 g, 99% yield). The product was characterized by 1H-NMR (200 MHz, CDCl3): δ 1.41 (s, 9H), 2.26 (m, 2H), 2.55 (m, 3H), 2.74 (m, 1H), 4.84 (br, 1H).LC-MS analysis showed [M+H]+ peak of 187.