Citric Acid → HCID 86710845、化合物
反応式
[CH3:1][N:2]([CH2:4]/[CH:5]=[CH:6]/[C:7]([NH:9][C:10]1[CH:11]=[C:12]2[C:25]([NH:26][C:27]3[CH:28]=[CH:29][C:30]([F:34])=[C:31]([Cl:33])[CH:32]=3)=[N:24][CH:23]=[N:22][C:13]2=[CH:14][C:15]=1[O:16][C@@H:17]1[CH2:21][O:20][CH2:19][CH2:18]1)=[O:8])[CH3:3].[C:35]([OH:47])(=[O:46])[CH2:36][C:37]([CH2:42][C:43]([OH:45])=[O:44])([C:39]([OH:41])=[O:40])[OH:38]>C(O)C>[CH3:1][N:2]([CH2:4]/[CH:5]=[CH:6]/[C:7]([NH:9][C:10]1[CH:11]=[C:12]2[C:25]([NH:26][C:27]3[CH:28]=[CH:29][C:30]([F:34])=[C:31]([Cl:33])[CH:32]=3)=[N:24][CH:23]=[N:22][C:13]2=[CH:14][C:15]=1[O:16][C@@H:17]1[CH2:21][O:20][CH2:19][CH2:18]1)=[O:8])[CH3:3].[C:35]([O-:47])(=[O:46])[CH2:36][C:37]([CH2:42][C:43]([O-:45])=[O:44])([C:39]([O-:41])=[O:40])[OH:38]参加物
4
実験手順
Ethanol (2 ml) was added to 100 mg (0.205 mmol) afatinib free base and the light yellow solution was stirred at room temperature. A solution of 39.4 mg (0.205 mmol) citric acid in 0.5 ml ethanol was added over the course of 2 min. Another 0.5 ml ethanol was added. Precipitation was observed and the mixture was stirred for 15 min. The solid was filtered, washed with 0.5 ml ethanol and dried on rotary evaporator at 50° C. for 2 h to give 80 mg (57%) of a light yellow solid.