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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1626114Generated: November 2, 2026

2-(Difluoromethoxy)aniline → [Bis-(4-methoxy-phenyl)-phenyl-methyl]-{(4R,5R)-4-[5-(2-difluoromethoxy-phenylamino)-2-fluoro-phenyl]-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-yl}-amine

https://huagongshe.com/reaction/1626114

Reaction equation

Participants

RoleNameHCIDCharge
Reactant2-(Difluoromethoxy)anilineHCID 934620—
Reactant[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]-amineHCID 71008920—
Product[Bis-(4-methoxy-phenyl)-phenyl-methyl]-{(4R,5R)-4-[5-(2-difluoromethoxy-phenylamino)-2-fluoro-phenyl]-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-yl}-amineHCID 7100882845%

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 2-(difluoromethoxy)aniline yielded the title compound (45% yield) as a pale yellow foam. MS (ISP): m/z=686.5 [M+H]+.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08785436B2
Source datasetuspto-grants-2014_07
ORD IDord-fad3f6cf2d1b479cbda3fa2486fb4b6d
Source noteuspto-grants-2014_07