Patent ID: 8487134
Filing Date: 2013-07-16
Classification: C07C,Y02P

Abstract:
1. A process for preparing acylated amphetamine, methamphetamine and dexamphetamine derivatives (V4 or V4a) or its salt comprising reacting a parent amine (V1) with a to be coupled acid (V2) or a salt of the to be coupled acid (V2), said acid (V2) further being optionally protected by protecting group(s) in the presence of an alkylphosphonic acid anhydride (V3) as coupling agent and cleaving the protecting group(s) if the acid (V2) was protected, said process being performed in a one-pot reaction or in two or more separate steps according to the following equation 1: wherein n and the radicals R1 to R5 have the following meaning: R1 is benzyl, mono-, di-, tri-lower-alkyl-substituted phenylmethyl, mono-, di- or tri-lower-alkoxy-substituted phenylmethyl, R2 is lower alkyl R3 is H or lower alkyl R4 is an amino acid radical or an amino acid radical wherein at least one amino group is protected with a protecting group, or is a substituted alkyl group different from the amino acid radical R5 is C1-C8-alkyl n is a number ranging from either 3 to 5 if (V3) is a cyclic anhydride or 3 to 1000 if (V3) is an open-chain oligomer, including if (V3) is a mixtures of different open-chain and/or cyclic anhydrides.