1-Methyl-3-aminopyrazole → (R)-N-(bis(4-methoxyphenyl)(phenyl)methyl)-6,6-difluoro-5-(2-fluoro-5-(1-methyl-1H-pyrazol-3-ylamino)phenyl)-5,7,7-trimethyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine

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Reaction Steps

Prepared in an analogous manner as described for intermediate A9A or A13A from (R)—N-(bis(4-methoxyphenyl)(phenyl)methyl)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine (intermediate A8B) (210 mg, 315 μmol) and commercially available 1-methyl-1H-pyrazol-3-amine [CAS no 1904-31-0] (62.4 mg, 629 μmol). The (R)—N-(bis(4-methoxyphenyl)(phenyl)methyl)-6,6-difluoro-5-(2-fluoro-5-(1-methyl-1H-pyrazol-3-ylamino)phenyl)-5,7,7-trimethyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine (174 mg, 80.9%) was obtained as a light yellow foam. MS (ISP): m/z=684 [M+H]+.

Provenance & Evidence