申请人:VASCULAR BIOGENICS LTD.
公开号:US20130237720A1
公开(公告)日:2013-09-12
Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids, are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorus-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby. Further disclosed is substantially pure 1-hexadecyl-2-(4′-carboxy)butyl-sn-glycero-3-phosphocholine (CI-201).
本发明揭示了一种新型的合成路线,非常适用于工业制备具有治疗益处的氧化磷脂。特别是,本发明揭示了一种高效制备具有甘油骨架和一个或多个氧化基团连接到甘油骨架上的化合物的新方法,这些方法不需要柱层析。此外,还揭示了一种将含磷基团(如磷酸盐基团)引入具有甘油骨架和由此形成的中间体的新方法。还揭示了基本纯的1-十六烷基-2-(4'-羧基)丁基-sn-甘油-3-磷酸胆碱(CI-201)。