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2,6-二甲基-4-(取代呋喃基)-1,4-二氢吡啶-3,5-二羧酸酯类化合物的合成 被引量:6

SYNTHESIS OF ALKYL 2,6—DIMETHYL—(SUBSTITUTED OR UNSUBSTITUTED FURYL)—1, 4—DIHYDROPYRIDINE—3, 5—DICARBOXYLATES
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摘要 以硝苯吡啶为代表的1,4-二氢吡啶类化合物是一种有效的钙拮抗剂,广泛用于治疗心绞痛、室上心律失常、高血压和外周血管性疾病,同时也用于进行放射配基结合实验,以深入了解人体中生理钙及钙通道的性质和功能。目前已用于临床的这类钙拮抗剂主要有硝苯吡啶、间硝苯吡啶和硝苯苄啶等。 Calcium antagonists are drugs that selectively block potential dependent Ca^(2+) -channel and inhibit Ca^(2+) withdrawal on cell membrane .These drugs are used to treat cardiovascular or cephalovascular diseases. 1,4- Dihydropyridine derivatives in comparison with other drugs, have higher potency and selectivity on Ca^(2+)- antagonists.They are vasodilators and hypotensives. In this paper,eleven new dihydropyridine derivatives were prepared with the method of Hantzsch and were characterized on the basis of elemental analysis, intrared spectroscopy (IR) and proton naclear magnetic resonance (~1HNMR).The solubility in water,stability to heat and Ca^(2+)-antagonistic activity of the new compounds were reported.
出处 《药学学报》 CAS CSCD 北大核心 1991年第5期375-378,共4页 Acta Pharmaceutica Sinica
关键词 二氢吡啶 二羧酸酯类 化合物 合成 Dihydropyridine compounds Hantzxch synthesis Calcium antagonists
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参考文献5

  • 1王振纲,药学学报,1985年,20卷,235页
  • 2乌锡康,有机人名反应集.1,1984年
  • 3李仲杰,西北大学学报,1983年,1期,58页
  • 4张宝恒,药学学报,1980年,15卷,118页
  • 5王进贤,科学通报,1966年,17卷,419页

同被引文献22

  • 1李光华.二氢吡啶类钙拮抗剂[J].中国药物化学杂志,1991,1(2):66-71. 被引量:4
  • 2陈修心 陈维洲 等.心血管药理学(第2版)[M].北京:人民卫生出版社,1998.214-214.
  • 3Luscher T F, Cosentino F. The classification of calcium antagonists and their selection in the treatment of hypertension, A reappraisal[J].Drugs, 1998, 55 (4): 509-517.
  • 4Abernethy D R, Schwartz J B. Calcium-antagonist drugs[J]. New England J Med, 1999, 341 : 1 447-1 457.
  • 5Godfraind T. Calcium antagonists and vasodilatation [J ]. PharmacolTher, 1994, 64 (1): 37-75.
  • 6Atwal K S, Rovnyak G C, Schwartz J, et al. Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-ary1-1,4- dihydro-6-methy1-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines [J]. J Med Chem, 1990, 33 (5) : 1 510-1 515.
  • 7Atwal K S, Rovnyak G C, Kimball S D, et al. Dihydropyrimidine calcium channel blockers. 2,3-substituted-4- aryl-1,4-dihydro-6-methyl-5-pyrimidineearboxylie acid esters as potent mimics ofdihydropyridines[J]. J Med Chem, 1990, 33 (9): 2629-2635.
  • 8Mandal P K, Misra A K. HC104-SiO2 Catalyzed multicomponent reactions for the synthesis of privileged heterocyclic structures [J].Lett Org Chem, 2006, 3 (11): 848-853.
  • 9Misra A K, Agnihotri G, Madhusudan S K. Microwave-induced eco-friendly solvent-free Biginelli reaction catalyzed by calcium chloride[J ]. Indian J Chem, 2004, 43B (9) : 2 018-2 020.
  • 10Gupta R, Gupta M, Paul S, et al. Silica-supported ZnCl2-A highly active and reusable heterogeneous catalyst for the one-pot synthesis of dihydropyrimidinones-t hiones [J]. Can J Chem, 2007, 85 (3): 197-201.

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