Morpholine → HCID 178434997, compound
Reaction equation
[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[C:12](/[CH:13]=[CH:14]/[C:15]3[CH:16]=[C:17]([C:20]([OH:22])=O)[NH:18][N:19]=3)=[C:11]([CH3:23])[O:10][N:9]=2)=[CH:4][CH:3]=1.[NH:24]1[CH2:29][CH2:28][O:27][CH2:26][CH2:25]1>>[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[C:12](/[CH:13]=[CH:14]/[C:15]3[CH:16]=[C:17]([C:20]([N:24]4[CH2:29][CH2:28][O:27][CH2:26][CH2:25]4)=[O:22])[NH:18][N:19]=3)=[C:11]([CH3:23])[O:10][N:9]=2)=[CH:6][CH:7]=1Participants
3
Procedure
As described for example 131 (step 3), 5-{(E)-2-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-yl]-vinyl}-2H-pyrazole-3-carboxylic acid was converted, using morpholine instead of thiomorpholine S,S-dioxide, to the title compound (18 mg, 33%) which was obtained as an off white solid. MS: m/e=383.2 [M+H]+.
Sources & evidence
- ORD record
- ord-5129b9f371d04de7a33a9440cb9900a1
- Source dataset
- uspto-grants-2012_04
- Patent number
- US08163728B2
Reaction notes
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