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CN102295569A 一种制备(S)-琥珀酸美托洛尔的方法 有权 转让

一种制备(S)-琥珀酸美托洛尔的方法
摘要：
本发明属于药物化学领域，具体涉及一种制备(S)-琥珀酸美托洛尔的方法。将4-羟基苯乙基甲醚、(R)-环氧氯丙烷泵入反应釜中，反应过程中将反应料液泵入装填除水剂的外循环除水系统中循环除水，制得的(S)-3-[4-(2-甲氧基乙基)苯氧基]-1,2-环氧丙烷与异丙胺反应得到(S)-美托洛尔碱基；将(S)-美托洛尔碱基与琥珀酸混合，即得(S)-琥珀酸美托洛尔。在第一步反应过程通过外循环除水装置使得反应过程中产生的水可以有效地被除去，降低(S)-3-[4-(2-甲氧基乙基)苯氧基]-1,2-环氧丙烷的损失，实现低能耗、简单、快捷地生产，得到第一步产物(S)-3-[4-(2-甲氧基乙基)苯氧基]-1,2-环氧丙烷的转化率大于90%，最终(S)-琥珀酸美托洛尔的收率大于75%，反应底物利用率明显提高。
摘要（英）：

Belonging to the field of pharmaceutical chemistry, the invention specifically relates to a method for preparing (S)-metoprolol succinate. The method comprises the steps of: pumping hydroxyphenylethyl methyl ether and (R)-chloropropylene oxide into a reaction vessel, and during the reaction process, pumping a reaction feed liquid into an external circulating dewatering system loaded with a dewatering agent for circulating dewatering, reacting the prepared (S)-3-[4-(2-methoxyethyl) phenoxyl]-1, 2-epoxypropane with isopropylamine so as to obtain an (S)-metoprolol base; mixing the (S)-metoprolol base with succinic acid, thus obtaining (S)-metoprolol succinate. During the first step of reaction in the invention, water generated in the reaction process can be effectively removed through the external circulating dewatering device, and the loss of (S)-3-[4-(2-methoxyethyl) phenoxyl]-1, 2-epoxypropane is reduced, thus realizing simple and fast production of low energy consumption. By the method of the invention, the conversion rate of the first step product (S)-3-[4-(2-methoxyethyl) phenoxyl]-1, 2-epoxypropane is over 90%, the final yield of (S)-metoprolol succinate is greater than 75%, and the utilization rate of the reaction substrate is obviously enhanced.

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