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二氢吡啶类构效关系的实验研究
【作者】 梅其炳;
【作者基本信息】 第四军医大学 , 药理学, 1992, 博士
【摘要】 1,4-二氢吡啶类(1,4-dihydropyridines,DHPs)是近二十年来引入医学和生物科学领域中最引人注目的一类化合物。对其药物化学及其药理学的研究不仅具有重要的理论意义,也具有重要的实用价值。为了进一步阐明DHPs C-3,C-5位取代基的构效关系,探讨C-4取代基对其光敏感性的影响,发掘光稳定、高效、长效、高选择性、低毒性DHPs类降压药物,本实验合成了32种DHPs衍生物;对其光稳定性,构效关系及其药理特性进行了初步研究。 一.1,4-二氢吡啶类的合成 1.2,6-二甲基-4-(呋喃或芳香基)-1,4-二氢吡啶-3,5-二羧酸酯的合成 本实验以醇和双乙烯酮为原料在三乙胺催化下合成了10种乙酰乙酸酯;再将这10种乙酰乙酸酯与氨作用,制备相应的3-氨基巴豆酸酯;并将其中几种乙酰乙酸酯与糠醛、间硝基苯甲醛、邻氯苯甲醛作用,合成2-乙酰基-3-(2-呋喃基、3-硝基苯基或2-氯苯基)丙烯酸酯。最后,采用一分子醛、一分子乙酰乙酸酯和一分子3-氨基巴豆酸酯(二步法),或将一分子2-乙酰基-3-(2-呋喃基、3-硝基苯基或2-氯苯基)丙烯酸酯与一分子3-氨基巴豆酸酯(三步法)进行Hanstszch反应合成了32种1,4-DHPs衍生物。在这些化合物之中,F2、F3、F5、F6、F7、
【Abstract】 The chemical compounds, 1,4-dihydropyridines. (1,4 -DHPs), have been proved to be one of the most important chemical classes introduced into medical and biological sciences over the past twenty years and studies on their chemical and pharmacological properties are of great theoretical as well as practical significance. In the present study, 32 derivatives of DHPs were synthesized and their photostability, structure-activity relationship and pharmacological characteristics were investigated so that the structure-activity relationship between the substituents, C-3 and C-5, and the effect of the substituents, C-4, on photosensitivity could be further elucidated.SYNTHESIS OF 1, 4-DIHYDROPYRIDINESI. Synthesis of 2, 6-dimethyl-4-furyl or aryl-1, 4-dihydro-3, 5-pyridinedicarboxylate In the first experiment in our series, ten acetoacetates were synthesized from alcohol and diketen e as catalysized by triethylamine and they were mixed with ammonia to prepare 3-aminocrotonate.Moreover, some of the synthesized acetoacetates were employed for the production of 2-acetyl-3-( 2- furyl, 3- nitrophenyl, or 2-chlorophenyl)propenate by reacting with furfuraldehyde, 3-nitrobenzaldehyde and 2-chlorbenzaldehyde, Finally, 32
- 【网络出版投稿人】 第四军医大学 【网络出版年期】2007年 02期
- 【分类号】R914
- 【下载频次】472