| R-兰索拉唑的合成新方法 |
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| 引用本文： | 李翔,刘丰良,聂作兵,李翠钦.R-兰索拉唑的合成新方法[J].广州化学,2014,39(4):61-64. |
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| 作者姓名： | 李翔 刘丰良 聂作兵 李翠钦 |
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| 作者单位： | 中南大学化学化工学院,湖南长沙,410083 |
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| 摘 要： | 2-氯甲基-3-甲基-4-（2,2,2-三氟乙氧基）吡啶盐酸盐和2-巯基苯并咪唑经缩合反应得到兰索拉唑硫醚;以L-亮氨酸经结构修饰得到的二齿手性氨基醇为催化剂、叔丁基过氧化氢为氧化剂,不对称氧化兰索拉唑硫醚得到R-兰索拉唑粗品。经分离纯化得到产物,e.e.值99.5%,两步反应总收率43.3%。产物经IR、MS、^1H-NMR、手性HPLC确证。
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| 关 键 词： | L-亮氨酸 手性氨基醇 不对称氧化 合成 R-兰索拉唑 |
Novel Synthetic Method of R-lansoprazole |
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| LI Xiang,LIU Feng-liang,NIE Zuo-bing,LI Cui-qin.Novel Synthetic Method of R-lansoprazole[J].Guangzhou Chemistry,2014,39(4):61-64. |
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| Authors: | LI Xiang LIU Feng-liang NIE Zuo-bing LI Cui-qin |
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| Institution: | LIU Feng-liang, LI Xiang, NIE Zuo-bing, LI Cui- qin (School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China) |
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| Abstract: | R-Lansoprazole was synthesized from 2-chloromethyl-3-methyl-4-（2,2,2-tri-fluoroethoxy）pyridine hydrochloride and 2-mercaptobenzimidazole by condensation and asymmetric oxidation, in which bidentate chiral amino alcohols from L-leucine derivatives as chiral catalyst, using tert-butyl hydroperoxide as oxidant converts. After the purification, optical purity was 99.5%, and with an overall yield of 43.3%. The product was characterized by IR, MS, 1H-NMR and chiral HPLC. |
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| Keywords: | L-leucine chiral animo alcohol asymmetric oxidation synthesis R-lansoprazole |
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