关于氨酰心胺的合成研究

The Study about Synthesis fo Atenolol

目的:通过采用新方法提高氨酰心胺的质量和收率。方法:以对羟基苯乙酰胺为原料合成氨酰心胺需经缩合、胺化两步反应。改进缩合方法后,提高了缩合物熔点;胺化反应采用水做溶媒,改善了反应性能和反应条件。结果:含量由96.78%提高到98.11%,收率由90.10%提高到97.30%,总收率为52.8%。结论:该合成路线简单实用,易在生产中推广。

Objective:Using the new method to improve the content and the yield of Atenolol.Mehtod:Atenolol was synthesized from 4-hydroxy phenytacetamide via the two-step chem.ical reactions,condensation and amination.After the method of condensation was im- proved,the mp of condensate increased.The amination could be carried out under a water system instead of anhydrous system as reported.Result:The content rosed up from 96.78% to 98.11%, the yield from 90.10% to 97.30%.The total yield was 52.85%.Conclusion:This new synthesis route is simple and useful,can be easily realized in the wide production.