Triethylamine → (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

Participants

Reaction Steps

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 (9.0 mmol) in dichloromethane (150 ml) was subsequently added at 0° C. NEt3 (18.0 mmol) and 4,4′-dimethoxytriphenylmethyl chloride (9.9 mmol) and stirring was continued at 22° C. for 2 h. The mixture was washed with saturated aqueous NH4Cl, the organic layer was dried, evaporated 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 (A8A) as a colorless foam. MS (ISP): m/z=639.3 [M+H]+and 641.4 [M+2+H]+.

Provenance & Evidence