| 4,6-二甲基-2-(2,2-二苯基-乙烯氧基)嘧啶的合成工艺研究 |
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| 引用本文： | 刘志友,叶俊杰,孟红,赵平. 4,6-二甲基-2-(2,2-二苯基-乙烯氧基)嘧啶的合成工艺研究[J]. 现代药物与临床, 2016, 31(12): 1877-1878. DOI: 10.7501/j.issn.1674-5515.2016.12.001 |
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| 作者姓名： | 刘志友 叶俊杰 孟红 赵平 |
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| 作者单位： | 天津市医药集团技术发展有限公司,天津,300193 |
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| 基金项目： | 天津市科技支撑计划重点项目（05YFGZGX03100） |
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| 摘 要： | 目的设计并合成安立生坦降解杂质4,6-二甲基-2-(2,2-二苯基-乙烯氧基)嘧啶。方法以3,3-二苯基-2,3-环氧丙酸甲酯为起始原料经水解、脱羧、开环、亲核取代反应定向合成目标化合物。结果合成目标化合物并经IR、1H-NMR、HRMS确证其结构;HPLC归一化法测得样品质量分数为99.5%。结论该杂质作为对照品用于安立生坦的质量研究工作。
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| 关 键 词： | 4,6-二甲基-2-(2,2-二苯基-乙烯氧基)嘧啶 安立生坦 亲核取代反应 合成 |
| 收稿时间： | 2016-07-15 |
Synthesis of 2-[(2,2-diphenylethenyl)oxy]-4,6-dimethylpyrimidine |
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| LIU Zhi-you,YE Jun-jie,MENG Hong and ZHAO Ping. Synthesis of 2-[(2,2-diphenylethenyl)oxy]-4,6-dimethylpyrimidine[J]. Drugs & Clinic, 2016, 31(12): 1877-1878. DOI: 10.7501/j.issn.1674-5515.2016.12.001 |
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| Authors: | LIU Zhi-you YE Jun-jie MENG Hong ZHAO Ping |
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| Affiliation: | Tianjin Pharmaceutical Tech-Development Co. Ltd., Tianjin 300193, China;Tianjin Pharmaceutical Tech-Development Co. Ltd., Tianjin 300193, China;Tianjin Pharmaceutical Tech-Development Co. Ltd., Tianjin 300193, China;Tianjin Pharmaceutical Tech-Development Co. Ltd., Tianjin 300193, China |
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| Abstract: | Objective To design and synthesize 2-[(2,2-diphenylethenyl)oxy]-4,6-dimethylpyrimidine, degradation impurity of ambrisentan. Methods Methyl 3,3-diphenyl-2,3-epoxypropionate was used as starting material to synthesize the target compound by hydrolysis, decarboxylation, open-loop, and nucleophilicsubstitution reactions. Results The target compound was synthesized and characterized by IR, 1H-NMR, HRMS data, and the purity was 99.5% by HPLC. Conclusion The impurity can be used as reference substance to study the quality of ambrisentan. |
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| Keywords: | 2-[(2,2-diphenylethenyl)oxy]-4,6-dimethylpyrimidine ambrisentan nucleophilicsubstitution reaction synthesis |
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