闫金花,张秀欣,杨宇鑫,钟启迪.化学通报,2020,83(8):735-740.
3-氰基-1,4-二氢吡啶衍生物的合成
Syntheses of 3-Cyano-1,4-dihydropyridine Derivatives
投稿时间:2020-03-22  修订日期:2020-05-11
DOI:
中文关键词:  1,4-二氢吡啶  合成  硼氢化钾  3-氰基吡啶
英文关键词:1,4-Dihydropyridine  Synthesis  Potassium borohydride  3-Cyanopyridine
基金项目:河北省教育厅青年基金项目(QN2019165)资助
作者单位E-mail
闫金花 华北理工大学药学院 唐山 063200  
张秀欣 华北理工大学药学院 唐山 063200  
杨宇鑫 华北理工大学药学院 唐山 063200  
钟启迪 华北理工大学药学院 唐山 063200 qidizhong@hotmail.com 
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中文摘要:
      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。
英文摘要:
      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.
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