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CN106518850A 一种匹莫苯丹的化学合成方法 失效 - 权利终止

一种匹莫苯丹的化学合成方法
摘要：
本发明公开了一种匹莫苯丹的化学合成方法，其步骤为：在混合有机溶剂中，在复合催化剂作用下，乙酰苯胺和2-甲基-3-甲氧羰基丙酰氯反应生成3-对乙酰氨基苯甲酰基丁酸甲酯，再与硝化试剂反应得到3-(4-乙酰氨基-3-硝基苯甲酰基)-丁酸甲酯，然后3-(4-乙酰氨基-3-硝基苯甲酰基)-丁酸甲酯在醇类溶剂中与碱回流反应得到3-(4-氨基-3-硝基苯甲酰基)-丁酸，3-(4-氨基-3-硝基苯甲酰基)-丁酸与水合肼回流反应得到4,5-二氢-5-甲基-6-(4-氨基-3-硝基苯基)-3(2H)-哒嗪酮，4,5-二氢-5-甲基-6-(4-氨基-3-硝基)-3(2H)-哒嗪酮在无水甲醇中与锌粉还原得到4,5-二氢-5-甲基-6-(3,4-二氨基苯基)-3(2H)-哒嗪酮，4,5-二氢-5-甲基-6-(3,4-二氨基苯基)-3(2H)-哒嗪酮与对甲氧基苯甲醛回流反应得到匹莫苯丹。本发明反应步骤少，操作安全方便，成本低。
摘要（英）：

The invention discloses a chemical synthesis method of Pimobendan. The method comprises steps as follows: acetanilide and 2-methyl-3-(chloroformyl)propionate react to produce 3-p-acetylaminobenzoyl methyl butyrate in a mixed organic solvent under the action of a composite catalyst, 3-p-acetylaminobenzoyl methyl butyrate reacts with a nitration reagent, 3-(4-acetamido-3-nitrobenzoyl)-methyl butyrate is produced and subjected to a reflux reaction with alkali in an alcohol solvent to produce 3-(4-amino-3-nitrobenzoyl) butyrate, 3-(4-amino-3-nitrobenzoyl) butyrate and hydrazine hydrate are subjected to a reflux reaction, 4,5-dihydro-5-methyl-6-(4-amino-3-nitrophenyl)-3(2H)-pyridazinone is produced and reduced with zinc powder in absolute methanol, 4,5-dihydro-5-methyl-6-(3,4-diaminophenyl)-3(2H)-pyridazinone is produced and subjected to a reflux reaction with p-anisaldehyde, and Pimobendan is obtained. The method comprises a few reaction steps, operation is safe and convenient, and the cost is low.

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