Efficient [5+1] Synthesis of 4-Quinolones by Domino Amination and Conjugate Addition Reactions of 1-(2-Fluorophenyl)prop-2-yn-1-ones with Amines
作者:Viktor Iaroshenko、Satenik Mkrtchyan、Alexander Villinger
DOI:10.1055/s-0032-1316826
日期:——
the intermediates were isolated. A catalyst-free synthetic approach is described for the synthesis of 4-quinolone derivatives through a tandem amination/conjugated Michael addition sequence of 1-(2-fluorophenyl)prop-2-yn-1-one derivatives. The [5+1]-cyclization proceeds efficiently at a high temperature under an inert atmosphere with lithium carbonate as a base, and it provides a practical route to
摘要 描述了通过1-(2-氟苯基)丙-2-yn-1-one衍生物的串联胺化/共轭迈克尔加成序列来合成4-喹诺酮衍生物的无催化剂合成方法。[5 + 1]-环化反应是在高温下在惰性气氛下以碳酸锂为碱有效进行的,它为生产各种范围的4-喹诺酮提供了一条可行的途径。详细研究了该机理,并分离了几种中间体。 描述了通过1-(2-氟苯基)丙-2-yn-1-one衍生物的串联胺化/共轭迈克尔加成序列来合成4-喹诺酮衍生物的无催化剂合成方法。[5 + 1]-环化反应是在高温下在惰性气氛下以碳酸锂为碱有效进行的,它为生产各种范围的4-喹诺酮提供了一条可行的途径。详细研究了该机理,并分离了几种中间体。