2-(5-硝基苯并咪唑基)乙腈合成工艺探讨  

Technological Process of the Synthesis of 2-( 5-nitrobenzimidazole) acetonitrile

作　　者：朱文山[1] 王艰[1] 许秀枝[1] 李柱来[1] 

机构地区：[1]福建医科大学药学院,福州350004

出　　处：《海峡药学》2015年第8期225-228,共4页Strait Pharmaceutical Journal

基　　金：福建省科技厅重点项目(2012Y0034);福建医科大学教授基金(JS10005);福建省自然科学基金项目(2013J01375)

摘　　要：目的通过正交试验法优化目标产物2-(5-硝基苯并咪唑基)乙腈合成工艺条件。方法根据3因素4水平正交试验设计,以5-硝基苯并咪唑和氯乙腈为原料,通过亲核取代反应合成目标产物,以反应转化率为指标,优化实验条件。目标化合物通过IR、1HNMR进行结构表征。结果以氢氧化钾为缚酸剂,乙酸乙酯为溶剂,反应时间8h,得到的目标化合物总得率最高(79.9%),且后处理简单。结论通过正交试验法优化2-(5-硝基苯并咪唑基)乙腈的合成,所得产物产率高、纯度好。OBJECTIVE To optimized condition on the synthesis of 2-（ 5-nitro-benzimidazole ） acetonitrile by orthogonal experiment.METHODS According to L9 （34 ） orthogonal experiment design,the target product 2-（5-ni-troben-zimidazole） acetonitrile was synthesized from the nucleophilic substitution reaction of 5-nitrobenzimidazole and chloroacetonitrile.Optimized experimental condition base on reaction conversion rate index,and the structure of syn-thetic compound determined by IR、1 H-NMR analysis.RESULTS The target compound had the higher rate （79.9%） with potassium hydroxide as bound acid,ethyl acetate as solvent,the reaction time was 8h,and the post-processing was simple.CONCLUSION The synthesis of target compound 2-（5-nitrobenzimidazole） acetonitrile by orthogonal experiment is high yield and good purity.

关 键 词：5-硝基苯并咪唑 氯乙腈 正交试验 工艺学 

分 类 号：R914.5[医药卫生—药物化学]