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一锅法合成泮托拉唑钠 被引量:1

A Single-pot Process for the Production of Pantoprazole Sodium
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摘要 将2-氯甲基-3,4-二甲氧基吡啶盐酸盐与5-二氟甲氧基-2-巯基-1H-苯并咪唑在碱性水溶液中反应制得中间体,直接将其萃取至二氯甲烷中,然后用NaClO进行氧化,接着成盐、精制得到泮托拉唑钠。研究了氧化反应温度、氧化剂用量及滴加速度对泮托拉唑纯度的影响,得出了较佳的氧化反应条件。在此条件下泮托拉唑钠的纯度可达99.7%以上,总收率可达78.3%。 The intermediate of 5-(difloromethoxy)-2-[(3,4-dimethoxy-2-pyridinyl)methyl]-thio-lH-benzimidazole was synthesized in the presence of inorganic base, then oxidized by using sodium hypochlorite to form pantoprazole. To the oxidation reaction, the effect of the reaction temperature, dosage of oxidant and the dropping speed of oxidant agent on the purity of pantoprazole was studied, and the optimized parameters tbr preparing pantoprazole sodium was obtained. Under this condition, the target compound was produced with a purity 99.7 % and yield 78.3 %
作者 薛琳 谭淑珍
出处 《广东化工》 CAS 2014年第17期27-28,共2页 Guangdong Chemical Industry
基金 湖南省教育厅资助科研项目(14A012)
关键词 泮托拉唑钠 质子泵抑制剂 合成 pantoprazole sodium proton pump inhibitor synthesis
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  • 1Kohl B,Sturm E,Rainer G.Fluoroalkoxy substituted benzimidazoles useful as gastric acid secretion inhibitors[P].US:4758579,1988-07-19. 被引量:1
  • 2Kromer W,Postius S,Riedel A,et al.BY1023/SK&F 96022 INN pantoprazole,A Novel Gastric Proton Pump Inhibitor,Potently Inhibits Acid Secretion But Lacks Relevant Cytochrome P450 Interactions[S].The American Society for Pharmacology and Experimental Therapeutics,1990,254(1):129-135. 被引量:1
  • 3Kohl B,Sturm EW,Simon A,et al.(H+,K+)-ATPase Inhibiting 2-[(2-Pyridylmethyl)sulfinyl] benzimidazoles,A Novel Series of Dimethoxypyridyl-Substituted Inhibitors with Enhanced Selectivity,The Selection of Pantoprazole as a Clinical Candidate[J].J Med Chem.1992,35:1049-1057. 被引量:1
  • 4Pietro A,Marcello R,Gabriele R,et al.Process for the preparation of pyridine compounds[P].US:7605268 B2,2009-10-20. 被引量:1
  • 5Rudy Laurent Maria,De Smaele Dirk,Stefan Marcel Herman.Improved process for preparing benzimidazole-type compounds[P].WO:03/008406 A1,2003-1-30. 被引量:1
  • 6Ashok,Kishor R,Palani M,et al.Process for preparation of pyridinylmethylsulfinyl benzimidazole compounds and pyridine intermediates[P].WO:2009/116072A2. 被引量:1
  • 7Mathad V T,Govindan S,Kolla N K,et al.An Improved and Single-Pot Process for the Production of Pantoprazole Substantially Free from Sulfone Impurity[J].Organic Process Research & Development,2004,8:266-270. 被引量:1
  • 8Caterina N,Eleonora P,Pietro A,et al.Process for the preparation of pantoprazole and salts thereof[P].US:7081534 B2,2006-7-25. 被引量:1
  • 9Ilya A,Marioara M.Processes for the preparation fo substituted 2-(2-pyridylmethyl)sulphinyl-1-H-benzimidazoles[P].US:2003/0036554A1,2003-2-20. 被引量:1
  • 10Serafettin.Pyridine benzimidazole sulfoxides with high purity[P].WO:2005/077936A1. 被引量:1

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