1-Methyl-4-(prop-2-yn-1-yl)benzene → (R)-5,5-Difluoro-4-[5-fluoro-2-(4-methyl-benzyl)-3H-indol-6-yl]-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine

Participants

Reaction Steps

In a manner analogous to that described in Example 39, the coupling and cyclisation reaction of (R)-4-(5-amino-2-fluoro-4-iodo-phenyl)-5,5-difluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine (intermediate B6.1) with 1-methyl-4-prop-2-ynyl-benzene yielded the title compound (73% yield) as a light green foam. MS (ISP): m/z=388.3 [M+H]+.

Provenance & Evidence