Triethyl orthoacetate → 3-(3-trifluoromethyl-4-morpholinophenyl)-2,6-dimethylpyrimidin-4(3H)-one
反応式
[NH2:1]/[C:2](/[CH3:23])=[CH:3]\[C:4]([NH:6][C:7]1[CH:12]=[CH:11][C:10]([N:13]2[CH2:18][CH2:17][O:16][CH2:15][CH2:14]2)=[C:9]([C:19]([F:22])([F:21])[F:20])[CH:8]=1)=[O:5].[C:24](OCC)(OCC)(OCC)[CH3:25]>>[F:20][C:19]([F:22])([F:21])[C:9]1[CH:8]=[C:7]([N:6]2[C:4](=[O:5])[CH:3]=[C:2]([CH3:23])[N:1]=[C:24]2[CH3:25])[CH:12]=[CH:11][C:10]=1[N:13]1[CH2:14][CH2:15][O:16][CH2:17][CH2:18]1参加物
3
反応条件
- 温度
- 150 °C
実験手順
A mixture of (Z)-3-amino-N-(3-trifluoromethyl-4-morpholinophenyl)but-2-enamide (4.0 g, 12.1 mmol) and triethyl orthoacetate (10 mL) was stirred at 150° C. overnight. The mixture was cooled to rt and concentrated in vacuo. The residue was purified by a silica gel column chromatography (PE/EtOAc (V/V)=1:1) to give the title compound as a pale yellow solid (3.00 g, 70%). The compound was characterized by the following spectroscopic data: