| 坎地沙坦西来替昔酯的合成工艺改进 |
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| 引用本文： | 朱彦民,景士云,王钝,吴秀静,宫平. 坎地沙坦西来替昔酯的合成工艺改进[J]. 中国药物化学杂志, 2003, 13(1): 31-33 |
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| 作者姓名： | 朱彦民 景士云 王钝 吴秀静 宫平 |
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| 作者单位： | 1. 哈尔滨制药集团制药总厂,黑龙江,哈尔滨,150086
2. 沈阳药科大学制药工程学院,辽宁,沈阳,110016 |
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| 摘 要： | 目的 完成坎地沙坦西来替昔酯(TCV-116)的合成，并得到文献报道的C-晶型产物。方法 设计了以3-硝基-1，2-苯二甲酸为起始原料，经酯比、氯化、Curtis重排、取代、还原、两步环合、酯基碱水解、酯化、转晶共10步反应，制备得到目标化合物的合成路线。结果与结论 制备得到目标化合物，与文献报道的合成路线相比，反应步骤简化，还原反应有改进。经红外、粉末X-射线衍射及热分析，证明产物晶型为C晶型。
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| 关 键 词： | 坎地沙坦西来替昔酯 合成工艺 改进 制备 药物化学 |
| 文章编号： | 1005-0108(2003)01-0031-03 |
Improvement of the synthetic procedure of candesartan cilexitil(TCV-116) |
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| ZHU Yan-min,JING Shi-yun,WANG Dun,WU Xiu-jing,GONG Ping. Improvement of the synthetic procedure of candesartan cilexitil(TCV-116)[J]. Chinese Journal of Medicinal Chemistry, 2003, 13(1): 31-33 |
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| Authors: | ZHU Yan-min JING Shi-yun WANG Dun WU Xiu-jing GONG Ping |
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| Affiliation: | ZHU Yan-min1,JING Shi-yun1,WANG Dun2,WU Xiu-jing2,GONG Ping2 |
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| Abstract: | Aim To synthesize candesartan cilexitil(TCV-116) and obtain a stable crystal as reported in the literature[1],C-type crystalline form of candesartan cilexitil.Methods Candesartan cilexitil was prepared from 3-nitro-1,2-benzenedicarboxylic acid via ten reactions,including esterification reaction,chlorination reaction,Curtis rearrangement,replacement reaction,etc.Results Candesartan cilexitil was successfully prepared and its crystalline form was confirmed to be C-type by IR,X-ray powder diffraction and DSC analysis.Conclusion Compared with that reported in the literature[1],the above synthetic route has been simplified and modifications were made in the reduction procedure. |
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| Keywords: | medicinal chemistry preparation process research candesartan cilexitil |
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