1-(Difluoromethyl)-1H-pyrazole-3-carboxylic acid → HCID 53240807, compound
Reaction equation
[NH2:1][C:2]1[CH:3]=[CH:4][C:5]([F:20])=[C:6]([C@:8]2([CH3:19])[C:13]([F:15])([F:14])[C:12]([CH3:17])([CH3:16])[O:11][C:10]([NH2:18])=[N:9]2)[CH:7]=1.[F:21][CH:22]([F:31])[N:23]1[CH:27]=[CH:26][C:25]([C:28](O)=[O:29])=[N:24]1>>[NH2:18][C:10]1[O:11][C:12]([CH3:16])([CH3:17])[C:13]([F:14])([F:15])[C@:8]([C:6]2[CH:7]=[C:2]([NH:1][C:28]([C:25]3[CH:26]=[CH:27][N:23]([CH:22]([F:31])[F:21])[N:24]=3)=[O:29])[CH:3]=[CH:4][C:5]=2[F:20])([CH3:19])[N:9]=1Participants
3
Procedure
The condensation of (R)-4-(5-amino-2-fluoro-phenyl)-5,5-difluoro-4,6,6-trimethyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine (intermediate XI-2) and 1-difluoromethyl-1H-pyrazole-3-carboxylic acid following procedure I yielded the title compound as a white solid. MS (ISP): m/z=432.2.
Sources & evidence
- ORD record
- ord-eb008c36931245dc92d3737de053cae5
- Source dataset
- uspto-grants-2013_03
- Patent number
- US08389513B2
Reaction notes
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