(4R,4aS,12bS)-4a-hydroxy-9-methoxy-3-methyl-2,4,7a,13-tetrahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one → Oxycodone

Participants

Reaction Conditions

Reaction Steps

72.50 kg of 14-Hydroxycodeinone is dissolved in 10% aqueous solution of acetic acid, 5% Pd/C catalyst is added, and the mixture is hydrogenated under overpressure of electrolytic hydrogen 104 to 106 kPa at temperatures 30 to 35° C. The reaction mixture is diluted with 200 l of water, filtered, the filtrate is cooled down to 5° C. and Oxycodone base is precipitated by adjusting pH with an addition of an ethanolic solution of ammonia to the value 9.2. The suspension is centrifuged, Oxycodone is washed with water and dried at 70 to 80° C. At least 67 kg (92%, purity 98.5%) of Oxycodone is obtained.

Provenance & Evidence