5-Chloro-2-thiophenecarboxylic acid → HCID 24760601、化合物
反応式
[Cl:1][C:2]1[S:6][C:5]([C:7]([OH:9])=O)=[CH:4][CH:3]=1.F[P-](F)(F)(F)(F)F.N1(O[P+](N(C)C)(N(C)C)N(C)C)C2C=CC=CC=2N=N1.[NH2:37][CH2:38][C:39]1[N:40]=[CH:41][N:42]([C:44]2[CH:53]=[CH:52][C:51]([N:54]3[CH:59]=[CH:58][CH:57]=[CH:56][C:55]3=[O:60])=[CH:50][C:45]=2[C:46]([O:48][CH3:49])=[O:47])[CH:43]=1>CN(C=O)C>[Cl:1][C:2]1[S:6][C:5]([C:7]([NH:37][CH2:38][C:39]2[N:40]=[CH:41][N:42]([C:44]3[CH:53]=[CH:52][C:51]([N:54]4[CH:59]=[CH:58][CH:57]=[CH:56][C:55]4=[O:60])=[CH:50][C:45]=3[C:46]([O:48][CH3:49])=[O:47])[CH:43]=2)=[O:9])=[CH:4][CH:3]=1参加物
5
実験手順
To a solution of 5-chlorothiophene-2-carboxylic acid 1-5 (40 mg, 0.25 mmol) and TEA (0.068 mL, 0.49 mmol) in DMF (2 mL), BOP (142 mg, 0.32 mmol) was added. After 5 min of mixing, the solution was added to the sample methyl 2-(4-(aminomethyl)-1H-imidazol-1-yl)-5-(2-oxopyridin-1(2H)-yl)benzoate prepared above. The mixture was then stirred at room temperature for 1 h before it was purified by HPLC to give the title compound (4 mg). MS 469.0 and 471.0 (M+H, Cl pattern).