1-(Morpholin-4-ylcarbonyl)-5-[4-(trifluoromethoxy)phenyl]piperidine-3-carboxylic acid → HCID 58002685, compound
Reaction equation
[N:1]1([C:7]([N:9]2[CH2:14][CH:13]([C:15]3[CH:20]=[CH:19][C:18]([O:21][C:22]([F:25])([F:24])[F:23])=[CH:17][CH:16]=3)[CH2:12][CH:11]([C:26]([OH:28])=O)[CH2:10]2)=[O:8])[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1.[Cl:29][C:30]1[S:34][C:33]([C:35](=[N:37]O)[NH2:36])=[CH:32][CH:31]=1>>[Cl:29][C:30]1[S:34][C:33]([C:35]2[N:37]=[C:26]([CH:11]3[CH2:12][CH:13]([C:15]4[CH:20]=[CH:19][C:18]([O:21][C:22]([F:23])([F:25])[F:24])=[CH:17][CH:16]=4)[CH2:14][N:9]([C:7]([N:1]4[CH2:2][CH2:3][O:4][CH2:5][CH2:6]4)=[O:8])[CH2:10]3)[O:28][N:36]=2)=[CH:32][CH:31]=1Participants
3
Procedure
80 mg (0.20 mmol) of 1-(morpholin-4-ylcarbonyl)-5-[4-(trifluoromethoxy)phenyl]piperidine-3-carboxylic acid (Example 44A) and 39 mg (0.22 mmol, 1.1 eq.) of 5-chloro-N′-hydroxythiophene-2-carboximidamide were reacted according to the General Method 1. Yield: 57 mg (53% of theory)
Sources & evidence
- ORD record
- ord-dd74bcc5991c4f9eb0bcb04dfffb5f98
- Source dataset
- uspto-grants-2012_02
- Patent number
- US08119663B2
Reaction notes
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