Patent ID: 9045456
Filing Date: 2015-06-02
Classification: A61P,C07D

Abstract:
1. A method for preparing an imatinib base of formula (1), comprising the steps of: (a) reacting a 4-[(4-methyl-1-piperazinyl)methyl]benzoic acid compound represented by the following formula (2) with a 2,2′-dibenzothiazolyl disulfide derivative represented by the following formula (5) in a reaction solvent selected from the group consisting of tetrahydrofuran, halogenated hydrocarbon, aromatic hydrocarbon, and mixtures thereof, in the presence of a phosphine derivative represented by the following formula (6), thereby preparing a thioester compound represented by the following formula (4); and (b) reacting the thioester compound represented by the following formula (4) prepared in step (a) with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyridine amine represented by the following formula (3) in a reaction solvent selected from the group consisting of tetrahydrofuran, halogenated hydrocarbon, aromatic hydrocarbon, and mixtures thereof, thereby preparing an imatinib base represented by the following formula (1), wherein the reaction solvent is toluene: wherein HA represents an acid; n is 0, 1 or 2; R and Z represent a phenyl group.