4-Methylmorpholine → HCID 69156110, compound

Participants

Reaction Steps

Isobutyl chloroformate (0.085 mL, 0.63 mmol) was added to a solution of (3R)-3-[(tert-butoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid (Intermediate 3, 210 mg, 0.63 mmol) and N-methylmorpholine (0.080 mL, 0.7 mmol) in 10 mL of dichloromethane at −20 to −30° C. and the resultant mixture was stirred for 1 h. A solution of (3R,7R)-3,7-dimethyl-1,4-diazepan-2-one in dichloromethane (5 mL) was added to the above solution. The reaction mixture was allowed to warm up to room temperature and stirring was continued overnight. The solution was subjected directly to flash chromatography on a Biotage® system (silica gel, 5% methanol/dichloromethane) to yield the title compound as a white solid. MS 358 (M−Boc+1).

Provenance & Evidence