2-(4-bromo-1H-imidazol-1-yl)-5-(trifluoromethyl)pyridine → [bis-(4-methoxy-phenyl)-phenyl-methyl]-((R)-6,6-difluoro-5-{2-fluoro-5-[1-(5-trifluoromethyl-pyridin-2-yl)-1H-imidazol-4-yl]-phenyl}-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl)-amine

Participants

Reaction Steps

Reaction of [bis-(4-methoxy-phenyl)-phenyl-methyl]-{(R)-5-[5-(5,5-dimethyl-[1,3,2]dioxaborinan-2-yl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl}-amine (intermediate B10.1) (300 mg, 380 μmol) with 2-(4-bromo-1H-imidazol-1-yl)-5-(trifluoromethyl)pyridine (111 mg, 380 μmol) yielded the [bis-(4-methoxy-phenyl)-phenyl-methyl]-((R)-6,6-difluoro-5-{2-fluoro-5-[1-(5-trifluoromethyl-pyridin-2-yl)-1H-imidazol-4-yl]-phenyl}-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl)-amine (77 mg, 25% yield) as a yellow foam. MS (ISP): m/z=800.3 [M+H]+.

Provenance & Evidence