申请人:HALPERIN Gideon
公开号:US20130079540A1
公开(公告)日:2013-03-28
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的合成路线,非常适用于工业制备治疗上有益的氧化磷脂。特别地,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附着在甘油骨架上的化合物的新方法,这些方法不需要柱层析。进一步揭示了一种引入含磷基团(如磷酸盐基团)到具有甘油骨架和由此形成的中间体的新方法。进一步揭示了几乎纯的1-十六烷基-2-(4'-羧基)丁基-sn-甘油-3-磷酸胆碱(CI-201)。