The method has the characteristics of being high in product yield, high in purity, low in impurity content, mild in reaction conditions, simple in operation, suitable for industrialized production and the like.read more read lessĪbstract: The present invention relates to a drug intermediate 15-ketone preparation method in chemical field. The preparation method comprises the following steps: in the presence of a first organic solvent, adopting N-4-7-4,6-quinazoline diamine as a raw material to have the acylation reaction with (E)-4-dimethyl amino crotonate hydrochloride to obtain an acylation reaction solution under the effect of thionyl chloride, water and alkaline water are added into the acylation reaction solution, the water phase is extracted by virtue of butyl acetate, an organic phase is collected, after the organic phase is washed, the organic phase is directly stirred and precipitated to obtain an afatinib crude product, then the afatinib crude product is refined to obtain a competitive product, and the competitive product reacts with maleic acid to obtain maleic acid afatinib. Abstract: The invention belongs to the technical field of synthesis of compounds, and relates to a preparation method of afatinib and maleate thereof.
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