反应详情

To a solution of 4-bromo-2-chloro-5-trifluoromethoxy-phenylamine (92.5 mg, 0.32 mmol) in DCM (0.82 mL) was added CDI (56.8 mg, 0.35 mmol). The reaction mixture was stirred at RT for 6 h and a solution of (S)-3-methyl-4-piperidin-4-yl-piperazine-1-carboxylic acid tert-butyl ester (99.3 mg, 0.35 mmol; Preparation 22) in DCM (1 mL) was added. The solution was concentrated under vacuum and purified by silica gel chromatography (0-5% MeOH/DCM). Product fractions were combined and concentrated under vacuum to provide the title intermediate (32 mg, 17% yield) as a clear oil. (m/z): [M+H]+ calcd for C23H31BrClF3N4O4 599.12, 601.11 found 601.4.

1. concentrationThe solution was concentrated under vacuum
2. custompurified by silica gel chromatography (0-5% MeOH/DCM)
3. concentrationconcentrated under vacuum