咪达那新的合成工艺研究  

Synthesis technology of imidafenacin

作　　者：郑其萍 郭颖娟[2] 丰艳梅[3] 

机构地区：[1]西安市第九医院,陕西西安710054 [2]陕西省中医药研究院汉唐制药有限公司,陕西西安710065 [3]西安交通大学医学院第二附属医院,陕西西安710004

出　　处：《现代药物与临床》2013年第6期819-821,共3页Drugs & Clinic

摘　　要：目的对咪达那新的合成工艺进行研究。方法以二苯乙腈为起始原料,与1,2-二溴乙烷经相转移反应生成4-溴-2,2-二苯基丁腈(1),化合物1在三乙胺存在下,于N,N-二甲基甲酰胺–二甲基亚砜中与2-甲基咪唑反应,生成4-(2-甲基-1H-咪唑-1-基)-2,2-二苯基丁腈(2),化合物2在70%硫酸溶液中,经水解、精制得咪达那新。结果该合成工艺总收率为40.2%,终产物质量分数为99.9%。结论工艺改进后,简化了操作过程,提高了咪达那新的收率。Objective To study the synthetic technology of imidafenacin. Methods Using 1,2-dibromomethane as the starting material, 4-bromo-2,2-diphenylbutyronitrile （1） was obtained after the phase transfer reaction with diphenylacetonitrile; compound 1 was then condensed with 2-methylimidazole in the presence of triethylamine in hot DMF-DMSO to obtain 4-（2-methyl-1-imidazolyl）- 2,2-diphenylbutyronitrile （2）. Imidafenacin was obtained according to the hydrolysis of compound 2 in the presence of 70% sulfuric acid. Results The total yield by the synthetic process was 40.2%, and the purity of imidafenacin was 99.9%. Conclusion After the improvement of the process, the operating process is simplified and the yield of imidafenacin is improved.

关 键 词：咪达那新 膀胱过度活动症 2-甲基咪唑 合成 

分 类 号：R914[医药卫生—药物化学]