【摘要】 以4-甲基-3-硝基苯胺为原料,先与取代的苯甲酰氯反应形成酰胺,再还原后与4-(3-吡啶基)嘧啶-2-胺偶联,最后成盐形成目标产物甲磺酸伊马替尼,总收率达到57.0%。产物结构经IR、1H NMR等确证。该方法原料易得,反应条件温和,危险性小,后处理简单,收率较高,生产成本降低,有利于工业化大生产。更多还原

【Abstract】 Using 4-methyl-3-nitroaniline as raw martial,Imatinib mesylate was synthesized by condensation,reduction,alkylation and salification with methane sulfonic acid,with the total yield of 57.0%.The structure of the target product was verified by IR and 1HNMR spectra.This synthetic route with lower cost and danger,mild reaction conditions and high yield,was worthy to have a further pilot manufacture.更多还原