5-Methanesulfonylthiophene-2-carboxylic acid → HCID 178504776, compound
Reaction equation
Cl.Cl.Cl.[O:4]1[C:8]2=[C:9]([N:13]3[CH2:18][CH2:17][N:16]([CH2:19][CH2:20][C@H:21]4[CH2:26][CH2:25][C@H:24]([NH2:27])[CH2:23][CH2:22]4)[CH2:15][CH2:14]3)[N:10]=[CH:11][CH:12]=[C:7]2[CH2:6][CH2:5]1.[CH3:28][S:29]([C:32]1[S:36][C:35]([C:37](O)=[O:38])=[CH:34][CH:33]=1)(=[O:31])=[O:30]>>[O:4]1[C:8]2=[C:9]([N:13]3[CH2:18][CH2:17][N:16]([CH2:19][CH2:20][C@H:21]4[CH2:26][CH2:25][C@H:24]([NH:27][C:37]([C:35]5[S:36][C:32]([S:29]([CH3:28])(=[O:31])=[O:30])=[CH:33][CH:34]=5)=[O:38])[CH2:23][CH2:22]4)[CH2:15][CH2:14]3)[N:10]=[CH:11][CH:12]=[C:7]2[CH2:6][CH2:5]1Participants
3
Procedure
The title compound, white solid (120 mg, 93%), MS (ISP) m/z=519.3 [(M+H)+], mp 212° C., was prepared in accordance with the general method of example 6 from trans-4-{2-[4-(2,3-dihydro-furo[2,3-c]pyridin-7-yl)-piperazin-1-yl]-ethyl}-cyclohexylamine trihydrochloride (intermediate B) (110 mg, 0.25 mmol) and 5-methanesulfonyl-thiophene-2-carboxylic acid.
Sources & evidence
- ORD record
- ord-859bb81d79d24b23affb8db194225980
- Source dataset
- uspto-grants-2013_06
- Patent number
- US08470828B2
Reaction notes
Loading…