Ethyl 2-amino-4-(4-bromophenyl)thiophene-3-carboxylate → 4-(4-Bromo-phenyl)-2-(2-ethoxycarbonyl-acetylamino)-thiophene-3-carboxylic acid ethyl ester
反応式
[CH2:1]([O:3][C:4]([C:6]1[C:10]([C:11]2[CH:16]=[CH:15][C:14]([Br:17])=[CH:13][CH:12]=2)=[CH:9][S:8][C:7]=1[NH2:18])=[O:5])[CH3:2].Cl[CH:20]([C:26]([O-])=[O:27])[C:21]([O:23][CH2:24][CH3:25])=[O:22]>C(Cl)Cl>[CH2:1]([O:3][C:4]([C:6]1[C:10]([C:11]2[CH:16]=[CH:15][C:14]([Br:17])=[CH:13][CH:12]=2)=[CH:9][S:8][C:7]=1[NH:18][C:26](=[O:27])[CH2:20][C:21]([O:23][CH2:24][CH3:25])=[O:22])=[O:5])[CH3:2]参加物
4
実験手順
To a solution of 2-amino-4-(4-bromophenyl)-thiophene-3-carboxylic acid ethyl ester (4.00 g, 11.5 mmol) in CH2Cl2 (40 mL) was added ethyl chloromalonate (2.15 g, 14.2 mmol) slowly. The mixture was then heated to reflux for 30 min. The mixture was concentrated under reduced pressure and separated by flash chromatography on silica gel (5–30% ethyl acetate in hexanes) giving the titled compound (4.98 g, 98.5%).