1-[(3-Hydroxyazetidin-1-yl)carbonyl]-5-[4-(trifluoromethyl)phenyl]piperidine-3-carboxylic acid → HCID 58002466, compound
Reaction equation
[OH:1][CH:2]1[CH2:5][N:4]([C:6]([N:8]2[CH2:13][CH:12]([C:14]3[CH:19]=[CH:18][C:17]([C:20]([F:23])([F:22])[F:21])=[CH:16][CH:15]=3)[CH2:11][CH:10]([C:24]([OH:26])=O)[CH2:9]2)=[O:7])[CH2:3]1.[F:27][C:28]1[C:29]([C:35](=[N:37]O)[NH2:36])=[N:30][CH:31]=[C:32]([F:34])[CH:33]=1>>[F:27][C:28]1[C:29]([C:35]2[N:36]=[C:24]([CH:10]3[CH2:11][CH:12]([C:14]4[CH:15]=[CH:16][C:17]([C:20]([F:21])([F:23])[F:22])=[CH:18][CH:19]=4)[CH2:13][N:8]([C:6]([N:4]4[CH2:3][CH:2]([OH:1])[CH2:5]4)=[O:7])[CH2:9]3)[O:26][N:37]=2)=[N:30][CH:31]=[C:32]([F:34])[CH:33]=1Participants
3
Procedure
90.0 mg (0.242 mmol) of 1-[(3-hydroxyazetidin-1-yl)carbonyl]-5-[4-(trifluoromethyl)phenyl]piperidine-3-carboxylic acid (Example 101A) and 61.0 mg (0.266 mmol) of 3,5-difluoro-N′-hydroxypyridine-2-carboximidamide were reacted according to the General Method 1. Yield: 24 mg (19% of theory).
Sources & evidence
- ORD record
- ord-c67d217444244a159a1dc5331956b0d2
- Source dataset
- uspto-grants-2012_02
- Patent number
- US08119663B2
Reaction notes
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