| 奥美沙坦酯关键中间体的合成工艺改进 |
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| 引用本文： | 刘存领,赵海桥,穆子齐. 奥美沙坦酯关键中间体的合成工艺改进[J]. 齐鲁药事, 2012, 0(10): 561-561,567 |
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| 作者姓名： | 刘存领 赵海桥 穆子齐 |
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| 作者单位： | [1]山东大学药学院,山东济南250012 [2]山东方明药业集团股份有限公司,山东菏泽274500 |
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| 摘 要： | 目的优化奥美沙坦酯关键中间体的合成工艺。方法以4-(1-羟基-1-甲基乙基)-2-丙基咪唑-5-羧酸乙酯为原料,与4-[2-(2-三苯甲基四唑-5-基)苯基]苄基溴缩合合成关键中间体4-(1-羟基-1-甲基乙基)-2-丙基-1-[2'-(三苯甲基四唑-5-基)联苯基-4-基甲基]咪唑-5-羧酸乙酯。结果与结论该优化的合成方法操作简便,制备的中间体收率为55%,质量较好。
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| 关 键 词： | 奥美沙坦酯 关键中间体 工艺改进 |
Improved synthesis of the key intermediate of olmesartan medoxomil |
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| LIU Cun-ling,ZHAO Hai-qiao,MU Zi-qi. Improved synthesis of the key intermediate of olmesartan medoxomil[J]. qilu pharmaceutical affairs, 2012, 0(10): 561-561,567 |
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| Authors: | LIU Cun-ling ZHAO Hai-qiao MU Zi-qi |
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| Affiliation: | 1. School of Pharmaceutical Sciences ,Shandong University ,Jinan 250012, China ;2. Shandong Fangming Pharmaceutical Group Co. ,Ltd. ,Heze 274500, China ) |
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| Abstract: | Objective To improve synthetic method of the key intermediate of olmesartan medoxomil. Methods 4 - （ 1 - hydroxy - 1 - methyl - ethyl ） - 2 - propyl - 1 - [ 2 - （ triphenylmethyl tetrazole - 5 - yl ） biphenyl - 4 - methyl ] imidazole - 5 - carboxylic acid ethyl ester was synthesized from 4 - （ 1 - hydroxy - 1 - methyl - ethyl ） - 2 - propylimidazole - 5 - earboxylate ethyl ester through condensation with 4 - [ 2 - （ 2 - （ triphenylmethyl ） tetrazole - 5 - yl ） phenyl ] benzyl bromide. Results and Conclusion The optimized synthesis method was simple with 55% yield of the intermediate and the quality was good. |
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| Keywords: | Olmesartan medoxomil Key intermediate Process improvement |
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