5-(4-Ethylphenyl)-1-(morpholin-4-ylcarbonyl)piperidine-3-carboxylic acid → 4-({3-(4-Ethylphenyl)-5-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}carbonyl)-morpholine
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][O:20][CH2:19][CH2:18]3)=[O:16])[CH2:12][CH:11]([C:23]([OH:25])=O)[CH2:10]2)=[CH:5][CH:4]=1)[CH3:2].O[C:27]1([C:34](=[NH:36])[NH2:35])[CH:32]=[CH:31][CH:30]=[C:29]([CH3:33])[CH2:28]1>>[CH2:1]([C:3]1[CH:4]=[CH:5][C:6]([CH:9]2[CH2:10][CH:11]([C:23]3[O:25][N:36]=[C:34]([C:27]4[CH:32]=[CH:31][CH:30]=[C:29]([CH3:33])[CH:28]=4)[N:35]=3)[CH2:12][N:13]([C:15]([N:17]3[CH2:18][CH2:19][O:20][CH2:21][CH2:22]3)=[O:16])[CH2:14]2)=[CH:7][CH:8]=1)[CH3:2]Participants
3
Procedure
69 mg (0.20 mmol) of 5-(4-ethylphenyl)-1-(morpholin-4-ylcarbonyl)piperidine-3-carboxylic acid (Example 38A) and 33 mg (0.22 mmol, 1.1 eq.) of 1-hydroxy-3-methylbenzenecarboximidamide were reacted according to the General Method 1. Yield: 16 mg (18% of theory)
Sources & evidence
- ORD record
- ord-a7b4253e760b4363b866a01aa86746d2
- Source dataset
- uspto-grants-2012_02
- Patent number
- US08119663B2
Reaction notes
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