| 新型双吲哚取代1，4-二氢吡啶类钙离子拮抗剂的合成 |
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| 引用本文： | 王倩,贺玲,刘永民,王静.新型双吲哚取代1，4-二氢吡啶类钙离子拮抗剂的合成[J].徐州医学院学报,2013,33(5):299-301. |
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| 作者姓名： | 王倩 贺玲 刘永民 王静 |
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| 作者单位： | 1. 徐州医学院生化与化学实验中心,江苏徐州,221002
2. 徐州医学院化学教研室 |
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| 基金项目： | 徐州医学院院长专项基金(项目编号：2010KJZ20)江苏省有机合成重点实验室开放课题(项目编号：KJS1010) |
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| 摘 要： | 目的设计合成一种新型结构1，4-二氢吡啶（1，4-DHP）钙离子通道拮抗剂：4-芳基-2，6-二吲哚基-3，5-二氰基-1，4-二氢吡啶。方法采用Hantzsch缩合反应，以芳香醛、3-氰乙酰基吲哚、醋酸铵为原料，微波辐射条件下三组分一锅法合成目标化合物。结果反应12～15min完成，产率76％～85％，所用产物均通过熔点（MP）、红外光谱（IR）和氢核磁共振谱（^1H NMR）等表征确认结构。结论本实验提供了一种新型1，4-DHP衍生物的合成方法，实现了对钙离子通道拈抗剂1，4-DHP的结构修饰，新化合物分子中含多个活性杂环骨架，具有潜在提高该类拮抗剂活性的意义。
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| 关 键 词： | 1，4-二氢吡啶 吲哚 合成 |
Synthesis of a new class of bis-indolyl substituted 1,4-DHP calcium antagonists |
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| WANG Qian
,
HE Ling
,
LIU Yongmin
,
WANG Jing.Synthesis of a new class of bis-indolyl substituted 1,4-DHP calcium antagonists[J].Acta Academiae Medicinae Xuzhou,2013,33(5):299-301. |
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| Authors: | WANG Qian HE Ling LIU Yongmin WANG Jing |
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| Institution: | 1. Experimental Center for Biochemistry and Chemistry, Xuzhou Medical College, Xuzhou, Jiangsu 221002, China; 2. Department of Chemistry, Xuzhou Medical College) |
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| Abstract: | Objective To develope a new method for synthesis of the title compounds, 4 - aryl - 2,6 - bis - indolyl -3,5 -dicyano- 1,4 -dihydropiperidines. Methods The target compounds were synthesized via one -pot muhicomponent reactions of 3 - cyanoacetyl indoles, aldehydes, and ammonium acetate under microwave irradiation condition. Results The reaction was completed in 12 - 15 min with yields of 76% - 85%. The structure of the products was determined by MP, IR,1H NMR spectra. Conclusion The article provides a new synthetic method of 1,4 - DHP derivatives. The products have many heterocyclic skeletons which are expected to exhibit enhanced biological activities. |
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| Keywords: | 1 4-dihydropiperidine indole synthesis |
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