tert-Butyl (3-aminopropyl)carbamate → N-(3-aminopropyl)-N-(4-(benzofuran-2-yl)thiazol-2-yl)thiophene-2-carboxamide
反応式
C(OC(=O)NCCCN)(C)(C)C.[O:13]1[C:17]2[CH:18]=[CH:19][CH:20]=[CH:21][C:16]=2[CH:15]=[C:14]1[C:22]1[N:23]=[C:24]([N:27]([CH2:35][CH2:36][CH2:37][NH:38]C(=O)OC(C)(C)C)[C:28]([C:30]2[S:31][CH:32]=[CH:33][CH:34]=2)=[O:29])[S:25][CH:26]=1.C(O)(C(F)(F)F)=O.ClCCl>>[NH2:38][CH2:37][CH2:36][CH2:35][N:27]([C:24]1[S:25][CH:26]=[C:22]([C:14]2[O:13][C:17]3[CH:18]=[CH:19][CH:20]=[CH:21][C:16]=3[CH:15]=2)[N:23]=1)[C:28]([C:30]1[S:31][CH:32]=[CH:33][CH:34]=1)=[O:29]参加物
4
実験手順
According to the procedure in Example 19, (3-amino-propyl)carbamic acid tert-butyl ester was transformed into tert-butyl 3-(N-(4-(benzofuran-2-yl)thiazol-2-yl)thiophene-2-carboxamido)propylcarbamate, which was reacted with TFA/dichoromethane (3:2), stirred at room temperature for 30 min, concentrated in vacuo, then dissolved in MeOH and treated with 1M HCl/ether. The resulting precipitate was filtered and dried in vacuo to provide N-(3-aminopropyl)-N-(4-(benzofuran-2-yl)thiazol-2-yl)thiophene-2-carboxamide (220 mg) as a white solid.