AN IMPROVED METHOD FOR THE SYNTHESIS OF NALOXONE

A new efficient route for the synthesis of naloxone is reported. Acetylation of 14-hydroxy-7,8-dihydrocodeinone with acetic anhydride and treatment of the resulting 14-acetoxy compound with cyanogen bromide gave 17-cyano derivative. Thelatter compound reacted with boron tribromide in chloroform yielding 14-acetoxy-17-cyano-7,8-dihydro-normorphinone, which after hydrolysis led to 14-hydroxy-7,8-dihydronormorphinone. N-allylation of the Secondary amine gave naloxone. The total yield was 53.3%. It appears that this method is better than those reported in the literature because of higher yield and simpler operation.