| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to an improved method of producing N-{5-[4-(4-methyl piperazinomethyl)benzoylamido]-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine amine of formula (I) (Imatibin) in form of a free base or acid addition salt. Said compounds have anti-tumour activity and can be used, for example, when treating leukaemia. The method involves reduction of N-(2-methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidine amine of formula (IV) in the presence of a chemical reducing agent, reaction of the obtained N-(2-methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidine amine of formula (II) with a dihydro-halide salt of 4-(4-methylpiperazinomethyl)benzoylhalide of formula (III) in the presence of an inert organic solvent which is not a base-acid acceptor to obtain a hydro-halide salt of imitinib of formula (I), where n equals 1, 2 or 3 and Hal denotes bromine, chlorine, fluorine or iodine in hydrated form, which, if needed, optionally undergoes further conversion to a free base or some other acid addition salt. ^ EFFECT: method simplifies the production and extraction process, the process takes place under mild conditions, the obtained hydrohalide salt of imatibin is virtually not soluble in organic solvents and can be easily extracted from the reaction mass. ^ 39 cl, 3 ex |
