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

Participants

Reaction Steps

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.

Provenance & Evidence