Diethyl Ether → 3-{[(3,4-Difluorophenyl)methyl]oxy}piperidine
反応式
[F:1][C:2]1[CH:3]=[C:4]([CH2:9][O:10][CH:11]2[CH2:16][CH2:15][CH2:14][N:13](C(OC(C)(C)C)=O)[CH2:12]2)[CH:5]=[CH:6][C:7]=1[F:8].C(OCC)C>CO>[F:1][C:2]1[CH:3]=[C:4]([CH2:9][O:10][CH:11]2[CH2:16][CH2:15][CH2:14][NH:13][CH2:12]2)[CH:5]=[CH:6][C:7]=1[F:8]参加物
4
反応条件
- 温度
- 2.5 °C
実験手順
1,1-dimethylethyl 3-{[(3,4-difluorophenyl)methyl]oxy}piperidine-1-carboxylate (Preparation 145, 3.38 g, 10.3 mmol) was dissolved in methanol (100 ml) and cooled 5 to 0° C., hydrogen chloride gas was bubbled into the reaction mixture for 3-5 min. The reaction mixture was concentrated in vacuo to give an oil, upon tituration with diethyl ether a white solid formed. The solid was separated by filtration to give the title compound (1.78 g, 65%) as the hydrochloride salt.