毕业论文 丙胺卡因合成工艺的研究.docVIP

学院代号 10716 学 号 101座机电话号码0 专业代码 100802 密 级 陕 西 中 医 学 院 Shaanxi University of Chinese Medicine 学士学位论文 丙胺卡因合成工艺的研究 中试 学位申请人 专业名称 制药工程（中药制药） 指导教师姓名 论文提交日期 2012年6月 摘 要 目的：本论文研究局麻药丙胺卡因的合成工艺，以确定最佳的合成工艺。方法：以2-氯丙酰氯和邻甲苯胺为起始原料经酰胺化后直接与正丙胺缩合两步反应制得丙胺卡因，在中间体的制备中主要考察是否加无水碳酸钾作为附酸剂，和附酸剂的对结果的影响。在丙胺卡因的制备中主要考查以丙酮，甲苯，正丙胺作溶剂对结果的影响，在丙酮和甲苯作溶剂时有对是否加加附酸剂和催化剂做了讨论。而以正丙胺做溶剂则对其用量进行讨论。最中确定了合成工艺。成果：本工艺减少了有机溶解的使用，缩短了反应时间。把合成的丙胺卡因收率从文献[1]中的60%提高到了80%，反应时间有14小时缩短至3小时。改进后的合成工艺收率高。操作方便适合工业化的生产。结果：丙胺卡因的最佳合成工艺是用正丙胺作溶剂，碳酸钾作附酸剂，石油醚：无水乙醇 8：1作丙胺卡因的重结晶溶剂。 关键字 丙胺卡因 ;合成;工艺路线; 局麻药 Abstract Objective: In order to determine the optimum synthesis process ,this paper studies synthesis process of local anesthetic prilcaine,. Methods: 2- Chloropropionyl chloride and o-toluidine as initial raw material through amidation and then directly condense with propylamine,all this need two steps. Which can result prilocaine. In the preparation of intermediates I mainly investigated whether add anhydrous potassium carbonate as Attached acid agent, and whether it has some effect on the result .In preparation of prilocaine , I test with acetone, toluene, n-propylamine as solvent in order known whether they have some effect on the outcome.when using acetone and toluene as solvent, I mainly discusse Attached acid agent and catalytic agent. .when using propylamine as solvent , I mainly discuss its dosage.all the discusses result the final process.adwantage: this process reduces the use of organic solution, shortens the reaction time.enhence the yield of Synthesis of prilocaine in literature [1] from 60% to 80%, reducing the reaction time from 14 hours to 3 hours.This improved synthetic process has the advantage of high yield ,convenient operation easy industrial production.Results: prilocaine optimum synthesis process using n-propylamine as solvent, potassium carbonate as Attached acid agent, using ethanol : water 8:1 as prilocaine recrystallization solvents, Keywords prilocaine; synthesis; proces