| R-(+)-兰索拉唑的合成研究 |
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| 引用本文： | 杜有国,宗在伟,陈祥峰. R-(+)-兰索拉唑的合成研究[J]. 化工时刊, 2010, 24(7): 17-18,24. DOI: 10.3969/j.issn.1002-154X.2010.07.005 |
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| 作者姓名： | 杜有国 宗在伟 陈祥峰 |
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| 作者单位： | 江苏奥赛康药业有限公司,江苏,南京,211112;江苏奥赛康药业有限公司,江苏,南京,211112;江苏奥赛康药业有限公司,江苏,南京,211112 |
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| 摘 要： | 2-氯甲基-3-甲基-4-(2,2,2-三氟乙氧基)吡啶盐酸盐经缩合兰索啦唑硫醚,再经不对称氧化制得R-兰索拉唑,粗品经纯化得到化学纯度99.6%,光学纯度99.8%的目标产物,总收率37.9%。反应条件温和,适合工业化生产。目标产物经元素分析、质谱、核磁共振及红外确认结构。
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| 关 键 词： | R-(+)-兰索拉唑 质子泵抑制剂 不对称氧化 合成 |
The Synthesis of R-(+)-lansoprazole |
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| Du Youguo,Zong Zaiwei,Chen Xiangfeng. The Synthesis of R-(+)-lansoprazole[J]. Chemical Industry Times, 2010, 24(7): 17-18,24. DOI: 10.3969/j.issn.1002-154X.2010.07.005 |
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| Authors: | Du Youguo Zong Zaiwei Chen Xiangfeng |
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| Affiliation: | Du Youguo Zong Zaiwei Chen Xiangfeng (Jingsu Aosaikang Pharmaceutical CO. , LTD. Jiangsu Nanjing 211112) |
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| Abstract: | R - （ ＋ ） - lansoprazole was synthesized from 2 - Chloromethyl - 3 - methyl - 4 - （2,2,2 - trifluoroethoxy） pyri - dine hydrochloride by condensation and asymmetric oxidation. By purifying, chemical purity of the product was 99.6% , optical purity was 99.8% , and with an overall yield of 37.9%. This synthetic process was under mild reactive conditions and with cheaper raw material. The process was suitable for industrial producing. The structure of R - （ ＋ ） lansop - razole was confirmed by MS, ^1H - NMR, ^13 C - NMRand IR. |
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| Keywords: | R - （ ＋ ） -lansoprazole proton pump inhibitor asymmetric oxidation synthesis |
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