1-(4-Fluorophenyl)pyrazole-4-boronic acid → [Bis-(4-methoxy-phenyl)-phenyl-methyl]-((4R,5R)-5-fluoro-4-{2-fluoro-5-[1-(4-fluoro-phenyl)-1H-pyrazol-4-yl]-phenyl}-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-yl)-amine

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]-[(4R,5R)-4-(5-bromo-2-fluoro-phenyl)-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-yl]-amine (intermediate C4.3) with 1-(4-fluorophenyl)-1H-pyrazol-4-ylboronic acid (CAS [1072945-89-1]) and tetrakis(triphenylphosphine)-palladium(0) as the catalyst yielded the title compound (75% yield) as a white foam. MS (ISP): m/z=689.3 [M+H]+.

Provenance & Evidence