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–aro...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.展开更多
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).
文摘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.
