PROCESS FOR THE PREPARATION OF 14-HYDROXY-N-ETHOXY-CARBONYL-NORCODEINONE AND NOROXYMORPHONE

摘要

N-ETHOXYCARBONYL-14-HYDROXY-NORCODEINONE IS PREPARED BY CONTACTING N-ETHOXYCARBONYL-NORCODEINONE DIENOL ACETATE WITH AN AROMATIC OR ALIPHATIC PEROXYGEN ACID, MONOBASIC OR POLYBASIC FOR A REACTICAL GROUP, SUBSTITUTE EFFECT FOR A REACET - SUBSTITUTION OH IN POSITION 14 OF NORCODEINONE DIENOL ACETATE. /P P IN A PREFERRED EMBODIMENT, THE REACTION CONDITIONS ARE SUCH THAT THE CONTACT TAKES PLACE: A. IN THE PRESENCE OF A MODERATELY STRONG ACID HAVING A KP OF ABOUT 0.3 TO ABOUT 3.5, B. IN THE PRESENCE OF AN INERT ORGANIC SOLVENT, AND C. IN THE PRACTICAL ABSENCE OF WATER. /P P CODEINE IS TRANSFORMED INTO NOROXYMORPHONE BY AN IMPROVED PROCESS USING THE ABOVE PROCESS TO INTRODUCE THE 14-HYDROXY GROUP IN THE CODEINE DERIVATIVE.