Invention Grant
US08697880B2 Compounds useful for the synthesis of S- and R-omeprazole and a process for their preparation 失效
可用于合成S-和R-奥美拉唑的化合物及其制备方法

  • Patent Title: Compounds useful for the synthesis of S- and R-omeprazole and a process for their preparation
  • Patent Title (中): 可用于合成S-和R-奥美拉唑的化合物及其制备方法
  • Application No.: US12329077
    Application Date: 2008-12-05
  • Publication No.: US08697880B2
    Publication Date: 2014-04-15
  • Inventor: Sverker Von UngeChristina Fregler
  • Applicant: Sverker Von UngeChristina Fregler
  • Applicant Address: SE Sodertalje
  • Assignee: AstraZeneca AB
  • Current Assignee: AstraZeneca AB
  • Current Assignee Address: SE Sodertalje
  • Agent David M. Gryte
  • Priority: SE0400410-7 20040220
  • Main IPC: C07D401/12
  • IPC: C07D401/12
Compounds useful for the synthesis of S- and R-omeprazole and a process for their preparation
Abstract:
The present invention relates to an improved method for the synthesis of the (S)- or (R)-enantiomer of omeprazole, characterized in that 2-[[(4-X-3,5-dimethylpyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole or 2-[[(4-X-3,5-dimethyl-1-oxidopyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole, wherein X is a leaving group, is oxidized into the corresponding sulphoxide which is obtained as a crystalline compound. Recrystallization of the thus obtained sulphoxide results in a compound of enhanced chemical and optical purity, which is subsequently transformed into the (S)- or (R)-enantiomer of omeprazole.
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