Patent ID: 8853401
Filing Date: 2014-10-07
Classification: A61P,C07D

Abstract:
1. A process for preparing intermediates useful in the synthesis of morphinane and morphinone compounds comprising: (a) reacting a compound of the formula (II) with a compound of the formula (III) under conditions to form compounds of the formulae R-(Ia) and S-(Ib): wherein R R R LG is a leaving group; PG is a protecting group; Z is a suitable counter anion; and each alkyl, alkylene and aryl is optionally fluoro-substituted and/or deuterated; and (b) isolating the compound of the formula R-(Ia); and (c) treating the remaining side products, including the compound of the formula S-(Ib) and a mixture of the compounds of the formulae R-(Ia) and S-(Ib) under N-demethylation conditions to form a compound of the formula (IV): wherein R R R PG is a protecting group; and each alkyl, alkylene and aryl is optionally fluoro-substituted and/or deuterated.