A metal‐free and base‐catalyzed cascade reaction of ortho‐(propargylamino)aryl ketones with primary alcohols, secondary amines, including various N‐heterocycles, and thiols through 1,4‐benzoxazepine intermediates was developed, providing a series of synthetically and medically valuable 3‐functionalized quinoline derivatives. The reaction process was easily manipulable and environmentally benign, producing 1.0 equiv. of water as the sole byproduct. Furthermore, bimolecular reactions for the synthesis of products containing two quinoline units were also succesful by utilizing this newly developed protocol.

中文翻译：

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邻（炔丙基氨基）芳基酮与N，O或S亲核试剂的碱催化级联反应，用于合成3功能化喹啉骨架。

开发了邻-（炔丙基氨基）芳基酮与伯醇，仲胺（包括各种N-杂环）和硫醇通过1,4-苯并氮杂pine中间体进行的无金属催化碱级联反应，提供了一系列合成和医学用途有价值的3功能化喹啉衍生物。反应过程易于操作且对环境无害，可产生1.0当量。水作为唯一的副产品。此外，利用这种新开发的方案，用于合成包含两个喹啉单元的产物的双分子反应也成功了。