Palladium-Catalyzed Acylation Reactions: A One-Pot Diversified Synthesis of Phthalazines, Phthalazinones and Benzoxazinones
作者:Basuli Suchand、Gedu Satyanarayana
DOI:10.1002/ejoc.201800159
日期:2018.5.24
proceeds through [Pd]‐catalyzed acylation and nucleophilic cyclocondensation with dinucleophilic reagents. This process was based on direct coupling with simple bench‐top aldehydes without the assistance of directing group and without activating the carbonyl group. The process is highly advantageous because it employs simple nitrogen‐based nucleophiles, and non‐toxic and readily accessible aldehydes as the
提出了一种用于酞嗪、酞嗪酮和苯并恶嗪酮多样化合成的连续单锅策略。该策略通过 [Pd] 催化的酰化和与双亲核试剂的亲核环缩合反应进行。该过程基于与简单的台式醛直接偶联,没有导向基团的帮助,也没有活化羰基。该方法非常有利,因为它使用简单的氮基亲核试剂和无毒且易于获得的醛作为羰基来源。最重要的是,该策略被应用于 PDE-4 抑制剂的一锅合成。