The invention relates to processes for preparing acylated amphetamine, methamphetamine and dexamphetamine derivatives by reacting the parent amine with the to be-coupled acid or a salt of the to-be coupled acid which acid is optionally protected, in the presence of an alkylphosphonic acid anhydride as coupling agent and, if the acid was protected then cleaving the protecting group(s), in a one-pot reaction or in two or more separate steps.