3-氨基-2-硝基吡啶置于tetrafluoroboric Acid体系中,用 甲苯 作为反应溶剂,化学反应生成 3-氟-2-硝基吡啶 参考文献:Cross-Coupling Reaction Of 2-Halo1-Methyl-1H-Imidazo[4,5-B]Pyridine Offers A New Synthetic Route To Mutagenic Heterocyclic Amine-Phip And Dmip 标题:Cross-Coupling Reaction Of 2-Halo1-Methyl-1H-Imidazo[4,5-B]Pyridine Offers A New Synthetic Route To Mutagenic Heterocyclic Amine-Phip And Dmip 摘要:杂环食品诱变剂 2-氨基-1-甲基-6-苯基咪唑并[4,5-B]吡啶 (Phip) 和 2-氨基-1,6-二甲基咪唑[4,5-B] 的改进合成方法] 吡啶 (Dmip) 已被报道.该路线重点介绍了 2-卤代-1-甲基-咪唑并[4,5-B]吡啶与二苯甲酮亚胺的优化钯催化 Buchwald 交叉偶联,然后进行酸水解,反应生成化合物 7.使用精心设计的条件,Suzuki 交叉偶联反应作为8的最后一步,使用高效催化系统在杂环核上引入芳基和甲基. DOI:10.5012/jkcs.2013.57.3.361
专利号:US-8362019-B2 优先权日:2008-02-01 标 题:Synthesis and anti-proliferative effect of substituted imidazo[4,5-b]pyrazine compounds 发明人:WINFIELD LEYTE L 权利人:SPELMAN COLLEGE; WINFIELD LEYTE L 摘要:This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyrazine compounds having the general formula n ntheir salts, pharmaceutical compositions, and methods of treatment using the subject compounds and compositions.
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参考文献:10.1055/s-0031-1290397 摘要:Eden J, Perkins D, Culshaw J, Ford S, Hayter B, Pike K. Synthesis of 3-Substituted 2-Aminopyridines via Displacement of 3-Fluoro-2-nitropyridine. Synlett. 2012 Jun 21;23(12):1816–20. doi: 10.1055/s-0031-1290397.