Invention Grant
US08735596B2 Process for producing crystals of polymorphic 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecaboxylic acid by poor-solvent addition method 有权
通过不良溶剂添加法生产多晶型2-(3-氰基-4-异丁氧基苯基)-4-甲基-5-噻唑可可酸的晶体的方法

  • Patent Title: Process for producing crystals of polymorphic 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecaboxylic acid by poor-solvent addition method
  • Patent Title (中): 通过不良溶剂添加法生产多晶型2-(3-氰基-4-异丁氧基苯基)-4-甲基-5-噻唑可可酸的晶体的方法
  • Application No.: US13382264
    Application Date: 2010-07-14
  • Publication No.: US08735596B2
    Publication Date: 2014-05-27
  • Inventor: Akihito UemuraTomoaki NogataTakumi Takeyasu
  • Applicant: Akihito UemuraTomoaki NogataTakumi Takeyasu
  • Applicant Address: JP Tokyo
  • Assignee: Teijin Pharma Limited
  • Current Assignee: Teijin Pharma Limited
  • Current Assignee Address: JP Tokyo
  • Agency: Sughrue Mion, PLLC
  • Priority: JP2009-166755 20090715
  • International Application: PCT/JP2010/062291 WO 20100714
  • International Announcement: WO2011/007895 WO 20110120
  • Main IPC: C07D277/34
  • IPC: C07D277/34
Process for producing crystals of polymorphic 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecaboxylic acid by poor-solvent addition method
Abstract:
Disclosed is a process for producing A-form crystals of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid, comprising: a step of dissolving by heating 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid in one or a plurality of solvents as a good solvent, selected from the group consisting of 1-propanol, 2-propanol, ethanol, and acetone; a step of cooling the solution; and a step of adding to the solution a hydrocarbon solvent as a poor solvent.
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