节点文献
倍他洛尔的合成工艺改进
Improved synthetic procedure of betaxolol
【摘要】 以对溴苯酚为原料 ,经苄基化、Grignard反应、烃化、脱苄基、烃化、胺化、成盐反应合成倍他洛尔 ,7步反应总收率为 2 1 8%。其结构经红外光谱、质谱、核磁共振氢谱、元素分析确证。在制备 4 [2 (环丙基甲氧基 )乙基 ] 1 苯甲氧基苯 (4 )中使用了相转移催化剂代替NaH ,收率达到 98%。化合物 4的脱苄反应 ,由加压反应改为常压反应 ,收率为 80 %。
【Abstract】 With 4-bromophenol as the starting material,the b et axolol was prepared through benzylation,Grignard reation,alkylation,debenzylatio n,alkylation,amination and salt formation.The overall yield was 21.8%.The struct ures were identified by IR ,MS, 1H-NMR and EA.The phase transfer catalys is instead of NaH in 98% yield in the preparation of compound 4.In the debenzylat ion reaction the normal pressure reaction substituted for the pressure reaction in the 80% yield.
【关键词】 药物化学;
工艺改进;
化学合成;
倍他洛尔;
对溴苯酚;
相转移催化;
【Key words】 medicinal chemistry; process improvement; chemical sy nthesis; betaxolol; 4-bromophenol; phase transfer catalysis;
【Key words】 medicinal chemistry; process improvement; chemical sy nthesis; betaxolol; 4-bromophenol; phase transfer catalysis;
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2004年05期
- 【分类号】TQ464
- 【被引频次】5
- 【下载频次】420