METHODS FOR ONE-POT N-DEMETHYLATION/N-ACYLATION OF MORPHINE AND TROPANE ALKALOIDS

摘要

Disclosed is a one pot method for the N-demethylation and N-acylation of a tertiary N-methylated heterocycle comprising reacting an N-methylated heterocycle substrate with an acylating agent reactant selected from the group consisting of an anhydride, a dicarbonate and a dicarbamic anhydride in the presence of a catalyst to obtain an N-acylated derivative product wherein the N-methylated heterocycle is a morphine alkaloid or a derivative thereof.