Ethyl Acetate → 1-[4-(2,3-Dihydro-benzofuran-2-yl)-piperidin-1-yl]-2,2,2-trifluoro-ethanone

反応式

O1C2=CC=CC2=CC=C1[CH:10]1[CH2:15][CH2:14][CH2:13][CH2:12][N:11]1[C:16](=[O:21])[C:17]([F:20])([F:19])[F:18].[C:22]([O:25][CH2:26][CH3:27])(=O)[CH3:23]>[Pd].CO>[O:25]1[C:26]2[CH:27]=[CH:12][CH:13]=[CH:14][C:15]=2[CH2:23][CH:22]1[CH:14]1[CH2:15][CH2:10][N:11]([C:16](=[O:21])[C:17]([F:18])([F:20])[F:19])[CH2:12][CH2:13]1

参加物

実験手順

A mixture of 1-(4-benzofuran-2-yl-piperidin-1-yl)-2,2,2-trifluoro-ethanone (11.50 g), 10% palladium on carbon (1.15 g), ethyl acetate (135 mL) and methanol (15 mL) is shaken under hydrogen atmosphere (3.5 bar) at room temperature for 24 h. The catalyst is then separated by filtration and the filtrate is concentrated to give an oil that is submitted to the next reaction without further purification. Yield: 11.12 g (crude); LC (method 2): tR=1.34 min.