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氨酰心安,化学名为4-(2-羟基-3-异丙胺基丙氧基)苯乙酰胺盐酸盐,为一种新的心脏选择性β-受体阻滞剂,而对血管和支气管的作用很小。与临床常用的心得安、心得宁比较,它具有二者的优点,克服了前者的无选择性和后者作用不强、副作用大的缺点。国外报道,本品为近年来一个较好的抗心律失常药物,其对高血压患者的心律失常的治疗效果优于其它β-受体阻滞剂。我们曾于1977年8月合成了本品的游离碱,以对-羟基苯乙酮为起始原料经三步反应,无需特殊试剂和设备。由于任务变动,未对其工艺条件继续进行考查,亦未进行临床考察。现将试制方法作简要介绍。合成路线
Atenolol, the chemical name for 4- (2-hydroxy-3-isopropylaminopropyloxy) benzene acetamide hydrochloride, is a new cardioselective β-blocker, while the blood vessels and Bronchial effect is small. Compared with the commonly used clinical experience, experience rather Ning, it has the advantages of both to overcome the former’s non-selectivity and the latter is not strong, the shortcomings of large side effects. Foreign reports, this product is a good anti-arrhythmic drugs in recent years, its effect on the treatment of arrhythmia in patients with hypertension than other β-blockers. We have in August 1977 synthesized the free base of this product, with - hydroxyacetophenone as the starting material through three steps, without special reagents and equipment. Due to the change of tasks, the process conditions were not continuously examined and no clinical investigation was conducted. Now trial production methods for a brief introduction. synthetic route