2-Chloro-5-cyanophenylboronic acid → 3'-((R)-2-{[Bis-(4-methoxy-phenyl)-phenyl-methyl]-amino}-5,5-difluoro-4,6,6-trimethyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-6-chloro-4'-fluoro-biphenyl-3-carbonitrile

Participants

Reaction Steps

In a manner analogous to that described in Example 9 a), the cross-coupling reaction of [bis-(4-methoxy-phenyl)-phenyl-methyl]-[(R)-4-(5-bromo-2-fluoro-phenyl)-5,5-difluoro-4,6,6-trimethyl-5,6-dihydro-4H-[1,3]oxazin-2-yl]-amine (intermediate C4.1) with 2-chloro-5-cyanophenylboronic acid yielded the title compound (22% yield) as a white foam.

Provenance & Evidence