反应详情

To a solution of (R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine (intermediate A7.1) (9.0 mmol) in dichloromethane (150 ml) was subsequently added at 0° C. triethylamine (18.0 mmol) and 4,4′-dimethoxytriphenylmethyl chloride (9.9 mmol) and stirring was continued at 22° C. for 2 hours. For the workup, the mixture was washed with saturated an aqueous solution of ammonium chloride. The organic layer was dried, evaporated at reduced pressure, and the residue was purified by chromatography on silica using cyclohexane/ethyl acetate to give pure (R)—N-(bis(4-methoxyphenyl)(phenyl)methyl)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine (A8.1) as a colorless foam. MS (ISP): m/z=639.3 [M+H]+ and 641.4 [M+2+H]+.

1. washFor the workup, the mixture was washed with saturated an aqueous solution of ammonium chloride
2. customThe organic layer was dried
3. customevaporated at reduced pressure
4. customthe residue was purified by chromatography on silica