99780-97-9

To a mixed methanol and triethylamine solution (9:1, 130 mL, v/v) of 3-aminopyrrolidin-2-one (39) (2.8 g, 28 mmol), di-tert-butyl dicarbonate (6.7 g, 30.8 mmol) was added. The reaction mixture was stirred overnight at room temperature and then heated to reflux for 2 hours. After completion of the reaction, the solvent was removed by distillation under reduced pressure and the resulting solid was collected by filtration and washed with ether to afford 3-(Boc-amino)pyrrolidin-2-one in 97% yield.

[1] Patent: US2005/165065, 2005, A1. Location in patent: Page/Page column 24
[2] Patent: WO2017/75056, 2017, A1. Location in patent: Paragraph 0371
[3] Journal of Medicinal Chemistry, 1986, vol. 29, # 2, p. 251 - 260
[4] Patent: US6441017, 2002, B1