Hydrogen Bromide → Galantamine Hydrobromide

Participants

Reaction Conditions

Reaction Steps

Total alkaloids (3.5 kg) containing 40% galanthamine, obtained according to example 1, are dissolved in 24 l of isopropanol. The solution, cooled to 0° C., is treated under stirring with 2.1 l of 48% aqueous hydrobromic acid, keeping the temperature during the addition between 0 and 5° C. The mixture is left under stirring at room temperature for three hours, then filtered and the solid is washed with some isopropanol and dried under vacuum at 70° C. 2.28 kg of galanthamine hydrobromide having HPLC purity of 85% are obtained. The resulting solid is suspended in 8 l of water, cooled to 0° C. and diluted with 5.5 l of 10% sodium carbonate. Seven extractions with 5 l of t-butyl acetate are carried out.

Provenance & Evidence