Hydrochloric Acid → [(R)-5-(5-amino-2-fluoro-phenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl]-[bis-(4-methoxy-phenyl)-phenyl-methyl]-amine

Participants

Reaction Conditions

Reaction Steps

To a solution of (R)—N-(bis(4-methoxyphenyl)(phenyl)methyl)-5-(5-(diphenylmethyleneamino)-2-fluorophenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine (intermediate A9A) (3.55 g, 4.8 mmol) in dioxane (100 ml) at 23° C. was added 1 M hydrochloric acid (4.8 ml, 4.8 mmol) and the mixture was stirred at 23° C. for 3 h. The reaction mixture was concentrated in vacuum and the residue was purified by silica gel flash chromatography with n-heptane/ethyl acetate to give the [(R)-5-(5-amino-2-fluoro-phenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl]-[bis-(4-methoxy-phenyl)-phenyl-methyl]-amine (1.45 g, 52%) as a white foam. MS (ISP): m/z=576.5 [M+H]+.

Provenance & Evidence