2-(4-Bromo-1H-imidazol-1-YL)pyridine → [bis-(4-methoxy-phenyl)-phenyl-methyl]-{(R)-6,6-difluoro-5-[2-fluoro-5-(1-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)pyridine [CAS 556775-77-0; J. Med. Chem. 47(19), 4645 (2004)) (111 mg, 494 μmol) yielded the [bis-(4-methoxy-phenyl)-phenyl-methyl]-{(R)-6,6-difluoro-5-[2-fluoro-5-(1-pyridin-2-yl-1H-imidazol-4-yl)-phenyl]-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl}-amine (71 mg, 25% yield) as a light red foam. MS (ISP): m/z=732.5 [M+H]+.

Provenance & Evidence