专利号:US-8173817-B2 优先权日:2004-05-28 标 题 :Stereoselective synthesis of benzimidazole sulfoxides 发明人:REDDY BANDI PARTHASARADHI; REDDY KURA RATHNAKAR; REDDY RAPOLU RAJI; REDDY DASARI MURALIDHARA 权利人:REDDY BANDI PARTHASARADHI; REDDY KURA RATHNAKAR; REDDY RAPOLU RAJI; REDDY DASARI MURALIDHARA; HETERO DRUGS LTD 摘要:The present invention relates to a process for stereoselective synthesis of substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]thio]-1H-benzimidazole is reacted with (R)-camphorsulfonyl chloride to form a mixture of 1-(R)-camphorsulfonyl-5- (and 6-)methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methylthio]-1H-benzimidazole, oxidized to obtain a diastereomeric excess of 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole over 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(R)-sulfinyl]-1H-benzimidazole, the diastereomers are separated by fractional crystallization and the separated 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is deprotected to give esomeprazole.
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-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-2006166986-A1 优先权日:2004-05-28 标题 :Novel stereoselective synthesis of benzimidazole sulfoxides
专利号:US-2011124634-A1 优先权日:2008-05-13 标 题:Bioactive compounds for treatment of cancer and neurodegenerative diseases 发明人:SUN CONNIE L; LI XIAOYUAN 权利人:PONIARD PHARMACEUTICALS INC 摘要:The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.
专利号:US-2008076930-A1 优先权日:2004-05-28 标题 :Novel stereoselective synthesis of benzimidazole sulfoxides
参考文献:10.3891/acta.chem.scand.42b-0524 摘要:Mittelbach M, Schmidt HW, Uray G, Junek H, Lamm B, Ankner K, Brändström A, Simonsson R. Synthesis of 4-methoxy-2,3,5-trimethylpyridine: a specific building block for compounds with gastric-acid inhibiting activity. Acta Chem Scand B. 1988 Sep;42(8):524–9. doi: 10.3891/acta.chem.scand.42b-0524.