An Improved First‐Generation Synthesis of ent‐Oxycodone

Abstract

AbstractAn improvement in the stereoselective total synthesis of unnatural (+)‐oxycodone from phenethyl acetate is described. The total step count was reduced by conducting some chemical transformations in “one‐pot” and a change in the sequence of chemical operations was implemented, in comparison with the previously published first‐generation synthesis. The synthesis of (+)‐oxycodone was completed in a total of 12 operations (17 steps) and an overall yield of 1.6%, in comparison to our previous synthesis (13 operations, 19 steps, 1.5% yield) Experimental and spectral data are provided for all new compounds.