2-(5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetic acid → HCID 58242748, compound
Reaction equation
[Cl-].[CH2:2]([O:4][C:5]([C:7]1[N:8]=[C:9]([CH:12]2[CH2:17][CH2:16][CH2:15][NH2+:14][CH2:13]2)[S:10][CH:11]=1)=[O:6])[CH3:3].[CH3:18][C:19]1[N:23]([CH2:24][C:25](O)=[O:26])[N:22]=[C:21]([C:28]([F:31])([F:30])[F:29])[CH:20]=1>>[CH3:18][C:19]1[N:23]([CH2:24][C:25]([N:14]2[CH2:15][CH2:16][CH2:17][CH:12]([C:9]3[S:10][CH:11]=[C:7]([C:5]([O:4][CH2:2][CH3:3])=[O:6])[N:8]=3)[CH2:13]2)=[O:26])[N:22]=[C:21]([C:28]([F:30])([F:29])[F:31])[CH:20]=1Participants
3
Procedure
3-[4-(Ethoxycarbonyl)-1,3-thiazol-2-yl]piperidinium chloride (VI-2, 5.32 g) is reacted analogously to Example IV-1 with [5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetic acid (4.00 g). This gives, after chromatographic purification, ethyl 2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-3-yl)-1,3-thiazole-4-carboxylate (5.7 g, 69%).
Workup
- customThis gives, after chromatographic purification, ethyl 2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-3-yl)-1,3-thiazole-4-carboxylate (5.7 g, 69%)
Sources & evidence
- ORD record
- ord-c28a185abcae4a5e92ef85ef11146e59
- Source dataset
- uspto-grants-2015_05
- Patent number
- US09029549B2
Reaction notes
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