4'-甲氧基乙酰苯胺置于盐酸,Tin,硫酸,硝酸,Potassium Hydroxide,Sodium Hydroxide体系中,用 甲醇,乙醇 用作溶剂,化学反应生成2-巯基-5-甲氧基苯并咪唑 参考文献:Diversified Synthesis Of Novel Quinoline And Dibenzo Thiazepine Derivatives Using Known Active Intermediates 标题:Diversified Synthesis Of Novel Quinoline And Dibenzo Thiazepine Derivatives Using Known Active Intermediates 摘要:新型药物的开发以控制常规药物治疗中抗药性感染是当今的需求.通过趋同合成法开发了少量与抗溃疡相关的衍生物.成功合成的衍生物包括二苯并噻嗪啶-吡啶(sln11-Sln15)和苯并咪唑-氢奎宁基衍生物(sln16-Sln20).在最终步骤中采用了微波,超声和常规技术进行耦合.有效的技术被识别为超声技术,主要体现在时间和产率上.报告的化合物通过元素分析和谱学研究(如1H,13C NMR和质谱)进行了结构表征. Doi:10.14233/ajchem.2013.14818
专利号:US-6437139-B1 优先权日:1997-05-06 标题 :Synthesis of pharmaceutically useful pyridine derivatives 发明人:ZOGHBI MICHEL; CHEN LIQUIN 权利人:PDI RES LAB INC 摘要:A process is provided for the preparation of compounds of formula I,useful in the preparation of compounds such as Omeprazole, Lansoprazole and Pantoprazole, wherein R1=H or CH3, R2=H or CH3, R3=Alkoxy (1-4C), OCH2CF3, Cyano, Hydrogen, Halogen, Acetoxy or Aryloxy, any electron withdrawing group or salts (organic or inorganic) of electron donating groups, R=Alkoxy, Hydroxy, Halogen, Activated ester, Tosylate, Mesylate, Thiol or Xanthyl, wherein the process for the preparation of compound of formula I employs a free radical reaction to functionalize the 2-position.
专利号:US-7683178-B2 优先权日:2002-10-18 标 题 :Method for the synthesis of a benzimidazole compound 发明人:GUSTAVSSON ANDERS 权利人:ASTRAZENECA AB 摘要:A process for the manufacture of omeprazole or esomeprazole from pyrmethyl alcohol via pyrmethyl chloride and pyrmetazole characterized in that the whole reaction sequence is carried out without any isolation or purification of intermediates. Further, the reaction is carried out in a solvent system common for the whole reaction sequence and inert to the reactants formed during the process and used in the process and comprises a water immiscible organic solvent and a specified amount of water.
专利号:WO-9840378-A1 优先权日:1997-03-07 标题 :Process for the preparation of 2-[[(2-pyridinyl)methyl]sulfinyl]-1h-benzimidazoles and novel compounds of use for such purpose 发明人:CLAUSEN FINN PRIESS; MCCLUSKEY KLAUS KARL; PREIKSCHAT HERBERT FRITZ; PEDERSEN SOEREN BOLS 权利人:BRISTOL MYERS SQUIBB CO; CLAUSEN FINN PRIESS; MCCLUSKEY KLAUS KARL; PREIKSCHAT HERBERT FRITZ; PEDERSEN SOEREN BOLS 摘要:2-[[(2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole derivatives of general formula (V) wherein R2 represents H, OCH¿3?, OCHF2 or CF3, R?3¿ represents H, CH¿3? or OCH3, R?4¿ represents H, OCH¿3?, OCH2CF3, halo or nitro, R?5¿ represents H, CH¿3? or OCH3, and n is 0 or 1, or salts thereof, are prepared by a new process proceeding via novel intermediates of general formulae (I), (II), (III) and (Va) wherein R?1¿ represents branched or straight C¿1-8?-alkyl, C3-8-cycloalkyl, aryl, aralkyl having 1-8 C-atoms in the alkyl moiety, or a 5- or 6-membered heterocyclic group having one, two or three hetero atoms selected from nitrogen, sulfur and oxygen in the heterocyclic ring. The compounds of formula (V) are biologically active and/or may be used as intermediates in the synthesis of biologically active compounds.
专利号:US-6121454-A 优先权日:1997-05-06 标题 :Synthesis of pharmaceutically useful pyridine derivatives 发明人:ZOGHBI MICHEL; CHEN LIQUIN 权利人:PDI RESEARCH LAB INC 摘要:A process is provided for the preparation of compounds of formula I, useful in the preparation of compounds such as Omeprazole, Lansoprazole and Pantoprazole, wherein R1=H or CH3, R2=H or CH3, R3=Alkoxy (1-4C), OCH2CF3, Cyano, Hydrogen, Halogen, Acetoxy or Aryloxy, any electron withdrawing group or salts (organic or inorganic) of electron donating groups, R=Alkoxy, Hydroxy, Halogen, Activated ester, Tosylate, Mesylate, Thiol or Xanthyl, wherein the process for the preparation of compound of formula I employs a free radical reaction to functionalize the 2-position.
专利号:US-8962851-B2 优先权日:2011-12-27 标题:One-pot process for the preparation of benzimidazole derivatives 发明人:DWIVEDI SHRIPRAKASH DHAR; PRASAD ASHOK; PAL DAYA RAM 权利人:CADILA HEALTHCARE LTD 摘要:The present invention discloses one pot process for enantioselective synthesis of single enantiomers of substituted sulphoxides 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles or said compounds in an enantiomerically enriched form.
专利号:WO-2004092142-A1 优先权日:2003-04-17 标 题:An improved process for manufacture of substituted benzimidazoles 发明人:VYAS KETAN DHANSUKHAL; SINGH DHARMENDRA; NANDAVADEKAR SANJAY; BHISE SANJAY; JADHAV ATUL; DESAI HEMAL 权利人:IPCA LAB LTD; VYAS KETAN DHANSUKHAL; SINGH DHARMENDRA; NANDAVADEKAR SANJAY; BHISE SANJAY; JADHAV ATUL; DESAI HEMAL 摘要:The present invention relates to a process for the production of benzimidazole derivatives comprising providing an amino acetamido benzene derivative; and condensing and cyclising the aminoacetamido benzene derivative in the presence of a base and in the presence of a cyclising agent under conditions effective to form the benzimidazole derivative. The acetamido benzene derivative has the formula (I) wherein R is OMe or OCHF2. The resulting substituted benzimidazoles are key intermediates in the synthesis of H<+>/K<+>-ATPase irreversible inhibitors, most particularly Omeprazole.
参考标题:Synthesis Of Novel Substituted 3-(4-((1H-Benzo[d]Imidazol-2-Ylthio)Methyl)-1-Phenyl-1H-Pyrazol-3-Yl)-2H-Chromen-2-Ones: Various Approaches 作者:Devulapally Srikrishna,Pramod Kumar Dubey |发布日期:2018.7 摘要:A Privileged Structure For Developing Probes Of Impressive Pharmacological Potentials, Some New Coumarin And Pyrazole Conjugates Of Benzimidazoles Were Synthesized With A Sulphur Linkage. Thus, 3-(2-Oxo-2 H -Chromen-3-Yl)-1-Phenyl-1 H -Pyrazole-4-Carbaldehyde ( 3 ) Was Prepared Starting From Simple Salicylaldehyde Which Has Been Used As An Important Synthon And Incorporated In A Series Of Structural
合成参考文献
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003). 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003). 摘要:Spitzner, D., Science of Synthesis, (2005) 15, 192.