A Step Beyond the Boundary of Traditional Aryne Chemistry

【作者】 李杨；

【Author】 Yang Li;School of Chemistry and Chemical Engineering,Chongqing University;

【机构】 重庆大学化学化工学院；

【摘要】 多取代苯环结构广泛存在于具有生物活性的天然产物、药物分子及有机功能材料结构中。如何高效快速地构建特定组合的多取代芳烃具有重要研究意义,也是合成有机化学的核心内容之一。虽然利用芳炔中间体可快速合成各种二取代芳烃,但传统单芳炔反应受到只能邻位双官能化的限制,无法有效发挥其在制备多取代芳环结构中的作用。本研究致力于突破上述研究限制,开发出1,2-苯二炔(多米诺苯炔)及简单芳炔参与的串联过程两条途径,实现了多种芳炔多官能化转化。此研究开发的手段可快捷合成多种药物分子,如抗卵巢癌药物Niraparib、治疗侏儒症药物Ibutamoren Mesylate、布洛芬类止痛药,及吲哚生物碱的合成。更多还原

【Abstract】 Polysubstituted arene structural motifs broadly exist in numerous natural products,drug molecules,and organic functional materials.How to quickly construct them continues to be one of the themes in organic chemistry.Although traditional benzyne intermediate can readily assemble vicinal difunctionalized arenes,it has been restricted to accomplish multifunctionalization with this highly active species.Our research focuses on the ways to break the limitation of traditional arene chemistry,which could be achieved via either 1,2-benzdiyne(namely domino aryne) chemistry or cascade simple aryne reaction/C-H functionalization.Meanwhile,we are interested in the discovery of new research maneuvers in aryne chemistry.Along with the development of our aryne multifunctionalization systems,several drug molecules could be prepared as well.更多还原