| 选择性胆固醇吸收抑制剂-依泽替米贝的合成工艺改进 |
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| 引用本文： | 刘毓宏,徐亮,黄铁强,戴连华.选择性胆固醇吸收抑制剂-依泽替米贝的合成工艺改进[J].广东化工,2011,38(5):144-145. |
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| 作者姓名： | 刘毓宏 徐亮 黄铁强 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： | 2008年广东省企业科技特派员行动计划专项项目 |
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| 摘 要： | 化合物7与1,3-丙二醇反应生成化合物8,与新戊酰氯和S-（＋）-4-苯基-2-噁唑烷酮反应生成化合物9,然后在钛化合物催化的条件下与化合物4反应生成化合物10,再成环生成具有β-内酰胺的化合物11,最后经CBS手性还原剂还原得到依泽替米贝。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。该合成路线短,反应条件温和,工艺操作简单,成本较低,收率和纯度较高,适合工业化生产。
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| 关 键 词： | 选择性胆固醇吸收抑制剂 依泽替米贝 合成 工艺 |
Selective Inhibitor of Cholesterol Absorption-an Improved Process for the Synthesis of Ezetimibe |
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| Liu Yuhong,Xu Liang,Huang Tieqiang,Dai Lianhua.Selective Inhibitor of Cholesterol Absorption-an Improved Process for the Synthesis of Ezetimibe[J].Guangdong Chemical Industry,2011,38(5):144-145. |
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| Authors: | Liu Yuhong Xu Liang Huang Tieqiang Dai Lianhua |
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| Affiliation: | (Enantiotech Co.,Ltd.,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: | selective Inhibitor of cholesterol absorption ezetimibe synthesis process |
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