4-Chloro-1-(2,2-difluoroethyl)-1H-pyrazole-3-carboxylic acid → 4-Chloro-1-(2,2-difluoro-ethyl)-1H-pyrazole-3-carboxylic acid [3-((4R,5R)-2-amino-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]amide

Participants

Role	Name	HCID	Charge
Reactant	4-Chloro-1-(2,2-difluoroethyl)-1H-pyrazole-3-carboxylic acid	HCID 19622801	—
Reactant	(4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine	HCID 86672006	—
Product	4-Chloro-1-(2,2-difluoro-ethyl)-1H-pyrazole-3-carboxylic acid [3-((4R,5R)-2-amino-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]amide	HCID 66559187	—

Reaction Steps

The condensation of (4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine (A8.3) and 4-chloro-1-(2,2-difluoro-ethyl)-1H-pyrazole-3-carboxylic acid (CAS 1006486-42-5) following procedure I yielded the title compound as a white solid. MS (ISP): m/z=448.2 [M+H]+.

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US08754075B2
Source dataset	uspto-grants-2014_06
ORD ID	ord-e0181c15b3f84f0ab7e578579da82510
Source note	uspto-grants-2014_06