Potassium Carbonate → 4-(6-fluoro-1-methyl-1H-indazol-3-yl)-1-(3-hydroxypropyl)piperidine

反応式

[F:1][C:2]1[CH:10]=[C:9]2[C:5]([C:6]([CH:12]3[CH2:17][CH2:16][NH:15][CH2:14][CH2:13]3)=[N:7][N:8]2[CH3:11])=[CH:4][CH:3]=1.C(=O)([O-])[O-].[K+].[K+].Br[CH2:25][CH2:26][CH2:27][OH:28]>CC(C)=O>[F:1][C:2]1[CH:10]=[C:9]2[C:5]([C:6]([CH:12]3[CH2:17][CH2:16][N:15]([CH2:25][CH2:26][CH2:27][OH:28])[CH2:14][CH2:13]3)=[N:7][N:8]2[CH3:11])=[CH:4][CH:3]=1

参加物

実験手順

A mixture of 4-(6-fluoro-1-methyl-1H-indazol-3-yl)piperidine (5.0 g; 0.02 mol), potassium carbonate (8.28 g; 0.06 mol), 3-bromopropanol (2.98 g; 0.02 mol) and acetone (100 ml) was stirred and refluxed for 20 h. The reaction mixture was filtered, concentrated in vacuo and purified by chromatography on silica gel 60 with ethyl acetate:methanol (8:2, v/v) as eluent. Concentration of the appropriate fractions afforded 2.1 g (34%) of 4-(6-fluoro-1-methyl-1H-indazol-3-yl)-1-(3-hydroxypropyl)piperidine.