Cyclopropylamine → HCID 58236588, compound

Participants

Reaction Conditions

Reaction Steps

To amine 126 (0.24 g, 0.46 mmol) in tetrahydrofuran (60 mL) at 0° C. was added triphosgene (0.054 g, 0.18 mmol) and the resulting solution was stirred for 1 h at 0° C. DIPEA (0.40 mL, 0.30 g, 2.3 mmol) and cyclopropylamine (0.26 g, 4.6 mmol) were sequentially added and the mixture was warmed to room temperature and stirred for 3 h, then concentrated under reduced pressure. The residue was partitioned between dichloromethane and water, the organic phase was collected, washed with sat. NH4Cl(aq) and brine, dried over MgSO4, filtered and concentrated. The residue was purified by flash chromatography on silica gel (ethyl acetate to 5% methanol/ethyl acetate), yielding 338 (0.19 g, 67% yield). MS (m/z): 608.4 (M+H).

Provenance & Evidence