📜2-Acetoxymethyl-4-Chloro-3,5-Dimethylpyridine置于盐酸体系中,用 水,乙酸乙酯 用作溶剂,以70.6%的收率获得埃索美拉唑杂质2
参考文献:A Process For The Preparation Of Omeprazol
标题:A Process For The Preparation Of Omeprazol
摘要:该过程首先是通过在催化剂存在下,将2,3,5-三甲基吡啶与过氧化氢反应,产生新的具有反应性的离子物种,从而大大减少所需步骤的数量.在最后一个重要步骤中,氧化成奥美拉唑时,使用了5-甲氧基-2-((3,5-二甲基-4-甲氧基-2-吡啶基)甲硫基)-1H-苯并咪唑的新盐,随着氧化的进行,沉淀出奥美拉唑.这种新的氧化方法避免了超氧化反应,实现了更快的氧化速度,高纯度和超过90%的收率.
专利信息
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:WO-9933807-A2
优先权日:1997-12-24
标 题 :Synthesis of pharmaceutically useful pyridine derivatives (intermediates) employing free radical substitution reactions to functionalize the 2-position of the pyridine
专利号:CA-2225863-A1
优先权日:1997-05-06
标 题 :Synthesis of pharmaceutical useful pyridine derivatives