反应详情

To a stirred solution of (1S,3S)-3-aminocyclopentanol (9.00 g, 89.0 mmol) (obtained from ASID pharmaceuticals) in DMF (45 mL) at RT under nitrogen was added DIPEA (31.0 mL, 178 mmol) followed by 1H-pyrazole-1-carboximidamide hydrochloride (14.7 g, 133 mmol). After stirring overnight Et2O (150 mL) was added and the reaction was stirred for 10 min. The Et2O was decanted and concentrated under high vacuum to afford 21 g (99%) of 1-((1S,3S)-3-hydroxycyclopentyl)guanidine (164) as a dark orange oil: MS m/z (APCI-pos) M+1=144.1

1. additionwas added
2. customThe Et2O was decanted
3. concentrationconcentrated under high vacuum