3-氰基-1,4-二氢吡啶衍生物的合成  

Syntheses of 3-Cyano-1,4-dihydropyridine Derivatives

作　　者：闫金花 张秀欣 杨宇鑫 钟启迪 Yan Jinhua;Zhang Xiuxin;Yang Yuxin;Zhong Qidi(College of Pharmacy,North China University of Science and Technology,Tangshan,063200)

机构地区：[1]华北理工大学药学院,唐山063200

出　　处：《化学通报》2020年第8期735-740,共6页Chemistry

基　　金：河北省教育厅青年基金项目(QN2019165)资助。

摘　　要：1,4-二氢吡啶类化合物具有多种生物活性,在临床上受到广泛应用,普遍用于各类心脑血管疾病的治疗。以3-氰基吡啶和含不同取代基的溴化苄为原料在加热回流15h的条件下合成中间体盐;以硼氢化钾(KBH4)作为还原剂,在冰水浴搅拌的情况下,与中间体盐反应,合成了15个结构新颖的1,4-二氢吡啶衍生物(a^o),产率可达85%~90%,其结构经1H NMR、13C NMR和质谱进行表征。该方法具有成本低、环境友好、操作简单、产率高的特点。1,4-dihydropyridine compounds have a variety of biological activities and are widely used in the treatment of various cardiovascular and cerebrovascular diseases.The intermediate salts were synthesized from 3-cyanopyridine and benzyl bromide containing different substituents under the condition of reflux for 15 hours.Potassium borohydride(KBH4)was used for the reduction of the intermediate salts in an ice-water bath,15 relatively novel 1,4-dihydrogen pyridine derivatives(a^o)were synthesized with the yield of 85%~90%.Their structures were characterized by 1H NMR,13C NMR and MS.The method has the characteristics of low cost,environmently friendly,easy operation and high yield.

关 键 词：1 4-二氢吡啶 合成 硼氢化钾 3-氰基吡啶 

分 类 号：O626.32[理学—有机化学]