Trifluoroacetic acid → 4(5-Chloro-2,3-methylenedioxypyrid-4-ylamino)-6-methoxy-7-(piperidin-4-ylmethoxy)quinazoline
反応式
FC(F)(F)C(O)=O.C(OC([N:15]1[CH2:20][CH2:19][CH:18]([CH2:21][O:22][C:23]2[CH:32]=[C:31]3[C:26]([C:27]([NH:33][C:34]4[C:39]([Cl:40])=[CH:38][N:37]=[C:36]5[O:41][CH2:42][O:43][C:35]=45)=[N:28][CH:29]=[N:30]3)=[CH:25][C:24]=2[O:44][CH3:45])[CH2:17][CH2:16]1)=O)(C)(C)C>C(Cl)Cl>[Cl:40][C:39]1[C:34]([NH:33][C:27]2[C:26]3[C:31](=[CH:32][C:23]([O:22][CH2:21][CH:18]4[CH2:19][CH2:20][NH:15][CH2:16][CH2:17]4)=[C:24]([O:44][CH3:45])[CH:25]=3)[N:30]=[CH:29][N:28]=2)=[C:35]2[O:43][CH2:42][O:41][C:36]2=[N:37][CH:38]=1参加物
4
反応物 2
生成物 1
試薬・触媒・溶媒 1
実験手順
Trifluoroacetic acid (1 ml) was added to a solution of 7-(N-tert-butoxycarbonylpiperidin-4-ylmethoxy)-4-(5-chloro-2,3-methylenedioxypyrid-4-ylamino)-6-methoxyquinazoline (0.253 g) in methylene chloride (10 ml) and the reaction mixture was stirred at ambient temperature for 1 hour. The reaction mixture was evaporated. Toluene was added to the residue and the mixture was evaporated. The residue was purified by column chromatography on silica (Isolute SCX column) using a 7M methanolic ammonia solution as eluent. There was thus obtained the title compound as a solid (0.187 g); NMR Spectrum: (DMSOd6) 1.25 (m, 2H), 1.75 (d, 2H), 1.93 (m, 1H), 2.54 (m, 2H), 3.0 (d, 2H), 3.93 (s, 3H), 3.98 (d, 2H), 6.17 (s, 2H), 7.15 (s, 1H), 7.76 (s, 1H), 7.78 (s, 1H), 8.23 (s, 1H); Mass Spectrum: M+H+ 444 and 446.