📜3-(4-(3-Methoxyphenoxy)-7H-Pyrrolo[2,3-D]Pyrimidin-6-yl)Aniline置于三溴化硼体系中,用 二氯甲烷 作为反应溶剂,以80%的收率获得产物3-[[6-(3-氨基苯基)-7H-吡咯并[2,3-D]嘧啶-4-基]氧基]苯酚 参考文献:Efficient Formation Of 4,6-Disubstituted Pyrrolo[2,3-D]Pyrimidines: A Novel Route To Tws119,A Glycogen Synthase Kinase-3β Inhibitor 标题:Efficient Formation Of 4,6-Disubstituted Pyrrolo[2,3-D]Pyrimidines: A Novel Route To Tws119,A Glycogen Synthase Kinase-3β Inhibitor 摘要:A Concise Synthesis Of 4,6-Disubstituted Pyrrolo[2,3-D]Pyrimidines Is Described. The Key Step Involves The Formation Of An Ether Or Thioether Linkage Along With Concurrent Ring Closure In One-Pot To Yield The Desired Product In Only Two Steps From A Common Intermediate. The Reaction Is Chemoselective To Incorporate Phenol,Thiophenol,And Thiol. This Method Enabled Efficient Production Of Tws119,A Glycogen Synthase Kinase-3 Beta Inhibitor. (C) 2010 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetlet.2010.05.032
专利号:US-11285169-B2 优先权日:2013-03-13 标题 :Methods for modulating chemotherapeutic cytotoxicity 发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R 权利人:US HEALTH 摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.
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