申请人:THE REGENTS OF THE UNIVERSITY OF COLORADO
公开号:US10912767B2
公开(公告)日:2021-02-09
The present invention includes compounds of the class anthracycline that have been modified to include photo-activated prodrug anthracycline compounds that are useful in the treatment of cancer. One example composition of the invention may include photodoxazolidine which may be synthesized in two steps from 4,5-dimethoxy-2-nitrobenzyl alcohol and doxazolidine. In this embodiment commercial 4,5-dimethoxyl-2-nitrobenzyl alcohol reacts with p-nitrophenylchloroformate to give the p-nitrophenyl carbonate of the benzyl alcohol derivative. The p-nitrophenyl carbonate is then reacted with doxazolidine to give the exemplary photodoxazolidine composition.
本发明包括经过修饰的蒽环类化合物,其中包括可用于治疗癌症的光活化原药蒽环类化合物。本发明的一种实例组合物可包括光恶唑烷,它可由 4,5-二甲氧基-2-硝基苯甲醇和多恶唑烷分两步合成。在本实施例中,商用 4,5-二甲氧基-2-硝基苯甲醇与对硝基苯基氯甲酸酯反应,生成苄醇衍生物的对硝基苯基碳酸酯。然后,对硝基苯碳酸盐与多沙唑烷反应,得到示例性光多沙唑烷组合物。