阿替洛尔的合成  

Synthesis of Atenolol

作　　者：崔艳霞 姜卫国 李淑芬 

机构地区：[1]东北制药总厂研究院

出　　处：《中国药物化学杂志》1996年第1期62-63,共2页Chinese Journal of Medicinal Chemistry

摘　　要：以对羟基苯乙酰胺为起始原料合成阿替洛尔需经缩合、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，提高了胺化物的质量和收率：含量由９６．７８％提高到９８．１１％，收率由９０．１０％提高到９７．３０％。胺化物经ＨＰＬＣ检测，达到了《英国药典》１９８８年版规定的标准，总收率为５２．８％。Atenolol was synthesized from 4-hydroxy phenylacetamide via the two-step chemical reactions, condensation and amination, After the method of condensation was improved, the mp of condensate increased from 167. 7～170. 0℃ to 172. 5～174. 0℃. The amination could be carried out under a water system instead of anhydrous system as reported by Spanish patent and German patent. As a result of this, the content rose up from 96. 78% to 98.11%, the yield from 90. 10% to 97.30%. After purification, its quality could reach the standards of BP 1988.The total yield was 52. 8%.

关 键 词：阿替洛尔 合成 对羟基苯乙酰胺 

分 类 号：TQ463.26[化学工程—制药化工]