4-Methylpyrazole → [Bis-(4-methoxy-phenyl)-phenyl-methyl]-{(4R,5R)-5-fluoro-4-[2-fluoro-5-(4-methyl-pyrazol-1-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 3 a), the amination 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 4-methyl-1H-pyrazole yielded the title compound (28% yield) as a white foam. MS (ISP): m/z=609.2 [M+H]+.

Provenance & Evidence