(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 Steps

The ratio of acid:14-hydroxycodeinone may be in the range of about 1:2.0 g/g to about 1:2.5 g/g, such as about 1:2.15 g/g. The ratio of 14-hydroxycodeinone:water may be in the range of about 1:0.005 to about 1:10, such as about 1:0.01 to about 1:3.13 g/g. The quantities of water and/or acid are not particularly limiting provided there is enough water and/or acid to substantially dissolve the 14-hydroxycodeinone. In this regard, the inventors have found that minimal water may be added to reaction mixture and the hydrogenation of 14-hydroxycodeinone has been successfully performed to produce oxycodone acid adduct having a low level of 6α-oxycodol when the quantity of water added corresponded only to amount which would have been present in the water-wet catalyst. The quantity of water present in the catalyst and/or 14-hydroxycodeinone (which may also be used wet) may be taken into account when calculating the total quantity of water to be used.

Provenance & Evidence