Tetrahydropyran-4-ylacetic acid → HCID 178520326, compound
Reaction equation
Cl.Cl.[F:3][C:4]1[C:12]2[O:11][CH:10]=[CH:9][C:8]=2[C:7]([CH:13]2[CH2:18][CH2:17][N:16]([CH2:19][CH2:20][C@H:21]3[CH2:26][CH2:25][C@H:24]([NH2:27])[CH2:23][CH2:22]3)[CH2:15][CH2:14]2)=[CH:6][CH:5]=1.[O:28]1[CH2:33][CH2:32][CH:31]([CH2:34][C:35](O)=[O:36])[CH2:30][CH2:29]1>>[F:3][C:4]1[C:12]2[O:11][CH:10]=[CH:9][C:8]=2[C:7]([CH:13]2[CH2:18][CH2:17][N:16]([CH2:19][CH2:20][C@H:21]3[CH2:22][CH2:23][C@H:24]([NH:27][C:35](=[O:36])[CH2:34][CH:31]4[CH2:32][CH2:33][O:28][CH2:29][CH2:30]4)[CH2:25][CH2:26]3)[CH2:15][CH2:14]2)=[CH:6][CH:5]=1Participants
3
Procedure
The title compound, off-white solid (76 mg, 65%), MS (ISP) m/z=471.4 [(M+H)+], mp 187.5° C., was prepared in accordance with the general method of example 1 from trans-4-{2-[4-(7-fluoro-benzofuran-4-yl)-piperidin-1-yl]-ethyl}-cyclohexylamine dihydrochloride (intermediate C) (104 mg, 0.25 mmol) and tetrahydropyran-4-yl-acetic acid.
Sources & evidence
- ORD record
- ord-56f078be10cc4adeacd8b33127655d1c
- Source dataset
- uspto-grants-2014_11
- Patent number
- US08877778B2
Reaction notes
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