Benzonitrile, 4-bromo- → 3'-((R)-3-{[bis-(4-methoxy-phenyl)-phenyl-methyl]-amino}-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-5-yl)-4'-fluoro-biphenyl-4-carbonitrile

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) (199 mg, 254 μmol) with 4-bromobenzonitrile (61.3 mg, 330 μmol) yielded the 3′-((R)-3-{[bis-(4-methoxy-phenyl)-phenyl-methyl]-amino}-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-5-yl)-4′-fluoro-biphenyl-4-carbonitrile (137 mg, 78% yield) as a white foam. MS (ISP): m/z=690.4 [M+H]+.

Provenance & Evidence