会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 8. 发明申请
    • SOLUTION SYNTHESIS OF PERIPHERAL ACTING ANALGESIC OPIOID TETRAPEPTIDES
    • 外周血白细胞介素四聚体的合成
    • WO1997007129A1
    • 1997-02-27
    • PCT/CA1996000552
    • 1996-08-15
    • BIOCHEM PHARMA INC.RINALDI, Nicholas
    • BIOCHEM PHARMA INC.
    • C07K05/107
    • C07K5/1016A61K38/00
    • This invention provides a bulk scale process for the solution synthesis of enantiomerically pure peripherally acting analgesic opioid tetrapeptides corresponding to formula (I): Tyr-(D)R1-R2-R3-NH2, where R1 is Ala or Arg; R2 is Phe or Phe(p-F); and R3 is Phe or Phe(p-F). A new and unique multi-step process is disclosed comprising the joining of two dipeptides using standard solution phase synthesis techniques, but adjusting the individual factors (e.g., solvents, activating agents, neutralizing agents etc.), to minimize racemization of the second amino acid. Tremendous cost efficiencies are achieved due to elimination of traditional sequential blocking-deblocking cycles and multiple chromatographic purification steps, which also enables these simple kilogram quantity methods to be scaled up to commercial production.
    • 本发明提供了用于溶液合成对应于式(I)的对映异构体纯的外用作用的镇痛阿片样四肽的大规模方法:Tyr-(D)R1-R2-R3-NH2,其中R1是Ala或Arg; R2是Phe或Phe(p-F); 且R3为Phe或Phe(p-F)。 公开了一种新的独特的多步骤方法,其包括使用标准溶液相合成技术连接两种二肽,但是调节各个因素(例如溶剂,活化剂,中和剂等),以使第二氨基酸的外消旋化最小化 。 由于消除了传统的顺序阻断 - 去封闭循环和多个色谱纯化步骤,从而实现了巨大的成本效率,这也使得这些简单的千克数量方法可以扩大到商业生产。