| HMG-CoA还原酶抑制剂-瑞舒伐他汀的合成研究 |
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| 引用本文： | 刘毓宏,戴连华. HMG-CoA还原酶抑制剂-瑞舒伐他汀的合成研究[J]. 广州化工, 2011, 39(8): 54-55 |
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| 作者姓名： | 刘毓宏 戴连华 |
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| 作者单位： | 中山奕安泰医药科技有限公司,广东中山,528437 |
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| 基金项目： | 中山市健康产业专项资金，中山市科技型中小企业技术创新基金 |
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| 摘 要： | 以4-(4-氟苯基)-6-异丙基-2-(N-甲基-N-甲磺酰基氨基)嘧啶-5-甲醇为起始原料,经缩合、水解去保护、酯化、水解、成钙盐等反应,重新设计并优化了缩合工艺和纯化工艺,制得降血脂药瑞舒伐他汀钙,合成的目标化合物,总收率为34.3%,纯度达到99.5%以上.并通过质谱、核磁共振氢谱和碳谱对目标产物进行了结构表征....
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| 关 键 词： | HMG-CoA还原酶抑制剂 瑞舒伐他汀钙 瑞舒伐他汀 合成 |
HMG-CoA Reductase Inhibitors-Study for Synthesis of Rosuvastatin Calcium |
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| LIU Yu-hong,DAI Lian-hua. HMG-CoA Reductase Inhibitors-Study for Synthesis of Rosuvastatin Calcium[J]. GuangZhou Chemical Industry and Technology, 2011, 39(8): 54-55 |
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| Authors: | LIU Yu-hong DAI Lian-hua |
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| Affiliation: | (Enantiotech Co.,Ltd.,Guangdong Zhongshan 528437,China) |
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| Abstract: | Starting with N-(5-((diphenylphosphoryl)methyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide(C28H29FN3O3PS),rosuvastatin calcium was prepared through condensation,hydrolysis and deprotection,esterification,hydrolysis,salting.The process was redesigned and the optimum technological conditions were investigated.Thus,the total yield reached 34.3%,HPLC purity 99%.The structure was determined by MS,CNMR and HNMR.The process exhibits simple,cost-efficient,high purity and yield,easy to scale up. |
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| Keywords: | HMG-CoA reductase inhibitors rosuvastatin calcium rosuvastatin synthesis |
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