5-Amino-2-chloropyridine → (R)-5-(5-(6-chloropyridin-3-ylamino)-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-one

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Reaction Steps

Prepared in an analogous manner as described for intermediate A9A or A13A from (R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-one (intermediate A16B) (200 mg, 546 μmol) and commercially available 5-amino-2-chloropyridine [CAS no 5350-93-6] (140 mg, 1.09 mmol). The (R)-5-(5-(6-chloropyridin-3-ylamino)-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-one (74 mg, 32.7%) was obtained as a light brown foam. MS (ISP): m/z=414.2 [(M+H)+] and 416.2 [(M+2+H)+].

Provenance & Evidence