1-(4-Benzyloxy-3-hydroxymethyl-phenyl)-2-(1,1-dimethyl-3-[1,2,4]triazol-1-yl-propylamino)-ethanol → 4-[2-(1,1-Dimethyl-3-[1,2,4]triazol-1-yl-propylamino)-1-hydroxy-ethyl]-2-hydroxymethyl-phenol
反応式
C([O:8][C:9]1[CH:14]=[CH:13][C:12]([CH:15]([OH:28])[CH2:16][NH:17][C:18]([CH3:27])([CH3:26])[CH2:19][CH2:20][N:21]2[CH:25]=[N:24][CH:23]=[N:22]2)=[CH:11][C:10]=1[CH2:29][OH:30])C1C=CC=CC=1>[Pd].CO>[CH3:27][C:18]([NH:17][CH2:16][CH:15]([C:12]1[CH:13]=[CH:14][C:9]([OH:8])=[C:10]([CH2:29][OH:30])[CH:11]=1)[OH:28])([CH3:26])[CH2:19][CH2:20][N:21]1[CH:25]=[N:24][CH:23]=[N:22]1参加物
4
実験手順
The debenzylation of 6 g of 1-(4-benzyloxy-3-hydroxymethyl-phenyl)-2-(1,1-dimethyl-3-[1,2,4]triazol-1-yl-propylamino)-ethanol is carried out hydrogenolytically with 1 g of palladium on charcoal (5%) in 100 mL methanol. After the catalyst has been removed by suction filtering and the filtrate has been evaporated down the residue is dissolved in 20 mL 90% ethanol, combined with sulphuric acid and seeded. The precipitated product is filtered off and washed. Yield: 3 g (55%, hemisulphate); m.p.=177-180° C.