Oxycodone → Oxycodone Hydrochloride

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Reaction Steps

A known amount of oxycodone (2.80 g) is charged into a 100 mL round-bottom flask equipped with a magnetic stirrer, a reflux condenser, and a thermometer. Into this, 11 g of anhydrous ethanol is added. This is heated to reflux to form a white suspension. Into this hot suspension, 2.75 g of hydrochloride-ethanol solution (4.85 M) is added in one portion. The resulting clear solution is stirred under reflux for 30 minutes. Heating is stopped and the solution is cooled initially to room temperature, and then to 0–5° C. for 2 h. A white precipitate of oxycodone hydrochloride is formed, which is isolated by filtration. The filter cake is washed with 7.8 g of 2-propanol and vacuum-dried for 3 h to yield oxycodone hydrochloride (2.634 g, 84%) of high purity (>99.5%). The amount of final product in the mother liquor corresponded to approximately 10% yield and the purity of the same is greater than 95%.

Provenance & Evidence