Transition-metal-free synthesis of 4-aminoisoquinolin-1(2H)-ones via a tandem reactionof arynes and oxazoles

查看全文 作　　者：Shaojun [1]Liu;Pei [1]Xie;Leifang [2]Wu;Jixing [2]Zhao;Zhihua [1]Cai;Lin [1]He 机构地区：[1]Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Bingtuan,School of Chemistry and Chemical Engineering,Shihezi University,Xinjiang Uygur Autonomous Region 832000,People’s Republic of China;[2]Analysis and Testing Center of Shihezi University,Xinjiang Uygur Autonomous Region,832000,China 出　　处：《Organic Chemistry Frontiers》索引2022年第9卷第6期,共6页 基　　金：supported by the National Natural Science Foundation of China(No.22161039);the Excellent Young Teachers Plan of Bingtuan(2017CB001 and CZ027203,CZ002203);the International Cooperation Project of Shihezi University(No.GJHZ201801). 摘　　要：A facile and transition-metal-free method for the synthesis of 4-amino isoquinolin-1(2H)-ones has beendeveloped. Arynes react with 4,5-disubstituted oxazoles through a tandem Diels–Alder reaction/dehydrogenation–aromatization/tautamerization process to produce 4-amino isoquinolin-1(2H)-ones in moderate to excellent yields. The reaction can be easily scaled up and the product can be transformed to isoquinoline derivatives efficiently. 关 键 词：synthesis TRANSITION