| 脂蛋白脂酶激活剂艾溴利平类似物的合成 |
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| 引用本文： | 刘举,王洋,周云鹏,姜明俊,王正,徐利锋.脂蛋白脂酶激活剂艾溴利平类似物的合成[J].合成化学,2012,20(2):210-213. |
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| 作者姓名： | 刘举 王洋 周云鹏 姜明俊 王正 徐利锋 |
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| 作者单位： | 辽宁大学药学院药物研究所,辽宁沈阳,110036 |
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| 摘 要： | 合成了两个新型的艾溴利平类似物——N-2 -硝基-4-氯苯基-4-(膦酸二乙酯基)甲基]苯甲酰肼(5,总收率28.1％)和N-2-四氮唑基-4-氯苯基-4-(膦酸二乙酯基)甲基]苯甲酰胺(7,总收率30.5％).以对氯甲基苯甲酸为原料,经酯化、水解和酰氯反应制得中间体4-(膦酸二乙酯基)甲基]苯甲酰氯(4)；4与2-硝基-4-氯苯肼盐酸盐反应合成了5.4先与2-氨基-5-氯苯腈反应制得N-2-氰基-4-氯苯基-4-(膦酸二乙酯基)甲基]苯甲酰胺(6)；6再与叠氮化钠反应合成了7.其结构经1 H NMR和IR表征.
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| 关 键 词： | 脂蛋白脂酶激活剂 艾溴利平 类似物 药物合成 |
Synthesis of Lipoprotein Lipase Activator Ibrolipim Analogs |
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| LIU Ju
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WANG Yang
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ZHOU Yun-peng
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JIANG Ming-jun
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WANG Zheng
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XU Li-feng.Synthesis of Lipoprotein Lipase Activator Ibrolipim Analogs[J].Chinese Journal of Synthetic Chemistry,2012,20(2):210-213. |
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| Authors: | LIU Ju WANG Yang ZHOU Yun-peng JIANG Ming-jun WANG Zheng XU Li-feng |
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| Institution: | (Pharmaceutical Institute,College of Pharmacy,Liaoning University,Shenyang 110036,China) |
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| Abstract: | Two novel Ibrolipim analogs,diethyl 4-2-(4-chloro-2-nitrophenyl)hydrazinecarbonyl]benzylphosphonate(5) with 28.1% total yield and 4-{4-chloro-2-(1H-tetrazol-5-yl)phenyl]carbamoyl}benzylphosphonate(7) with 30.5% total yield,were synthesized.The intermediate diethyl 4-(chlorocarbonyl)benzylphosphonate(4) was prepared by esterification,hydrolysis and chlorination reaction from 4-(chloromethyl)benzoic acid.5 was obtained by the reaction of 4 with(4-chloro-2-nitrophenyl)hydrazine hydrochloride.7 was obtained by the reaction of 4 with 2-amino-5-chlorobenzonitrile,and then reaction with sodium azide in toluene.The structures were characterized by 1H NMR and IR. |
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| Keywords: | lipoprotein lipase activator Ibrolipim analogs drug synthesis |
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