5-(4-Ethylphenyl)-1-[(4-hydroxypiperidin-1-yl)carbonyl]piperidine-3-carboxylic acid → HCID 58002510, compound
Reaction equation
[CH2:1]([C:3]1[CH:8]=[CH:7][C:6]([CH:9]2[CH2:14][N:13]([C:15]([N:17]3[CH2:22][CH2:21][CH:20]([OH:23])[CH2:19][CH2:18]3)=[O:16])[CH2:12][CH:11]([C:24]([OH:26])=O)[CH2:10]2)=[CH:5][CH:4]=1)[CH3:2].O[N:28]1[CH:32]([C:33]([F:36])([F:35])[F:34])[N:31]([CH3:37])[C:30]([C:38](=[NH:40])[NH2:39])=[N:29]1>>[CH2:1]([C:3]1[CH:4]=[CH:5][C:6]([CH:9]2[CH2:10][CH:11]([C:24]3[O:26][N:40]=[C:38]([C:30]4[N:31]([CH3:37])[C:32]([C:33]([F:36])([F:35])[F:34])=[N:28][N:29]=4)[N:39]=3)[CH2:12][N:13]([C:15]([N:17]3[CH2:22][CH2:21][CH:20]([OH:23])[CH2:19][CH2:18]3)=[O:16])[CH2:14]2)=[CH:7][CH:8]=1)[CH3:2]Participants
3
Procedure
80 mg (0.22 mmol) of 5-(4-ethylphenyl)-1-[(4-hydroxypiperidin-1-yl)carbonyl]piperidine-3-carboxylic acid (Example 59A) and 70 mg (0.33 mmol) of 1-hydroxy-4-methyl-5-(trifluoromethyl)-4H-1,2,4-triazole-3-carboximidamide were reacted according to the General Method 2. Yield: 37 mg (30% of theory)
Sources & evidence
- ORD record
- ord-15829d186dd94263991093a17870e29f
- Source dataset
- uspto-grants-2012_02
- Patent number
- US08119663B2
Reaction notes
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