苯佐卡因的合成资料.docVIP

药物化学大实验（论文） 学 生 姓 名： 指 导 教 师： 专 业： 药 学 学 院： 药 学 院 2014年 6 月 27 日 摘要 苯佐卡因是一种重要的医药中间体，用于合成奥索仿、奥索卡因、普鲁卡因等。同时，它在医药上又用于局部麻醉剂。本文研究了以对硝基苯甲酸和乙醇为原料，经酯化、还原两步骤制备苯坐卡因的工艺。 首先，采用三种方法合成硝基苯甲酸甲酯。以对甲苯磺酸为催化剂，利用常规加热方法合成对硝基苯甲酸乙酯，反应时间2.5h，产率95.1% 其次，以上一步制备的对硝基苯甲酸乙脂为原料，Fe粉为还原剂，并加入适量电解质氯化铵，还原制备苯佐卡因，产率84%。 本文探讨了醇酸摩尔比，催化剂用量，反应温度，反应时间对对硝基苯甲酸乙酯产率的影响；同时优化Fe粉还原工艺，总结出制备苯佐卡因的最佳工艺条件。产物通过红外光谱、核磁共振、物理分析等方法证实与目标产品一致。 关键词：苯佐卡因；对硝基苯甲酸乙脂；对甲苯磺酸；酯化；还原 ABSTRACT Benzocaine is an important medicinal intermediate products of Orthoform,Orthocaine and Procaine,and is also one of local anesthetics.The preparation of Benzocaine by esterification and reduction from 4-Nitrobenzonic acid and Ethanol has been intensively studied. First. The synthesis of p-Nitro-ethylbenzoate by three method.p-Nitro-ethylbenzoate was synthesized by conventional heating method,using p-toluene sulfonic acid as catalyst.thereaction time was 2.5h and the yield was 95.1% Secondly iron and ammonium chloride were used for the synthesis of benzocaine from P-Nitro-ethylbenzoate,the yield was 84% In the paper ,effects of molar ratio of alcohol and acid,catalyst,reaction temperature ,reaction time on yield of the P-Nitro-ethylbenzoate were studied ,while the reduction process was improved.Finally it conclude optimal conditions for the prepare of benzocaine. Key Words: benzocaine; P-Nitro-ethylbenzoate; esterification; reduction 摘要 1 ABSTRACT 2 1.1 苯佐卡因的概况 3 1.1.1 苯佐卡因的性质 3 1.1.2 苯佐卡因的用途 3 1.1