2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylic Acid → 2-[4-(2-Oxo-2h-3,1-benzoxazin-1(4h)-yl)piperidin-1-yl]-4-(trifluoromethyl)pyrimidine-5-carboxylic acid
Reaction equation
Cl.[NH:2]1[CH2:7][CH2:6][CH:5]([N:8]2[C:13]3[CH:14]=[CH:15][CH:16]=[CH:17][C:12]=3[CH2:11][O:10][C:9]2=[O:18])[CH2:4][CH2:3]1.Cl[C:20]1[N:25]=[C:24]([C:26]([F:29])([F:28])[F:27])[C:23]([C:30]([OH:32])=[O:31])=[CH:22][N:21]=1>>[O:18]=[C:9]1[O:10][CH2:11][C:12]2[CH:17]=[CH:16][CH:15]=[CH:14][C:13]=2[N:8]1[CH:5]1[CH2:4][CH2:3][N:2]([C:20]2[N:25]=[C:24]([C:26]([F:28])([F:29])[F:27])[C:23]([C:30]([OH:32])=[O:31])=[CH:22][N:21]=2)[CH2:7][CH2:6]1Participants
3
Procedure
The title compound was prepared from 1-piperidin-4-yl-1,4-dihydro-2H-3,1-benzoxazin-2-one hydrochloride (0.70 g) and 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylic acid (1.8 g) using the method of example 115 step (ii). Yield 1.1 g.
Sources & evidence
- ORD record
- ord-d8e8f080c7fa428a8799b33f6706aba9
- Source dataset
- uspto-grants-2004_11
- Patent number
- US06812226B2
Reaction notes
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