(R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine → HCID 86660426, compound

HRID 1186205Notes

Reaction equation

HRID 1186205 reaction equation
[NH2:1][C:2]1[CH:3]=[CH:4][C:5]([F:19])=[C:6]([C@:8]2([CH3:18])[C:14]([F:16])([F:15])[CH2:13][O:12][CH2:11][C:10]([NH2:17])=[N:9]2)[CH:7]=1.[F:20][C:21]([F:34])([F:33])[CH2:22][O:23][C:24]1[N:29]=[C:28]([C:30]([OH:32])=[O:31])[CH:27]=[N:26][CH:25]=1>>[CH:30]([OH:32])=[O:31].[NH2:17][C:10]1[CH2:11][O:12][CH2:13][C:14]([F:15])([F:16])[C@:8]([C:6]2[CH:7]=[C:2]([NH:1][C:30]([C:28]3[CH:27]=[N:26][CH:25]=[C:24]([O:23][CH2:22][C:21]([F:34])([F:33])[F:20])[N:29]=3)=[O:31])[CH:3]=[CH:4][C:5]=2[F:19])([CH3:18])[N:9]=1

Participants

3

Reactant 2

HCID 58562966(R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amineHCID 66456273HCID 66456273, compound

Product 1

HCID 86660426HCID 86660426, compound

Procedure

The coupling of (R)-5-(5-amino-2-fluorophenyl)-6,6-difluoro-5-methyl-2,5,6,7-tetrahydro-1,4-oxazepin-3-amine (intermediate A10A) and 6-(2,2,2-trifluoro-ethoxy)-pyrazine-2-carboxylic acid (prepared according to Suzuki, Y. et al., Int. Patent Application Publ. No. WO2009091016) yielded the title compound as an off-white solid. MS (ISP): m/z=478.1 [M+H]+.

Sources & evidence

ORD record
ord-89dae3bd392e4831bca05a0606a6e0c9
Source dataset
uspto-grants-2014_03
Patent number
US08673894B2

Reaction notes

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