作者:Jimena E Díaz、Silvia Ranieri、Nadia Gruber、Liliana R Orelli
DOI:10.3762/bjoc.13.145
日期:——
allows for the preparation of 3,4- and 1,4-dihydroquinazolines with different substitution patterns from 2-aminobenzylamine (2-ABA) as common precursor. The required functionalization of both amino groups present in 2-ABA was achieved by different routes involving selective N-acylation and cesium carbonate-mediated N-alkylation reactions, avoiding protection/deprotection steps. The heterocycles were efficiently
提出了一种直接合成二氢喹唑啉的策略,该策略允许从2-氨基苄胺(2-ABA)作为常见前体制备具有不同取代模式的3,4-和1,4-二氢喹唑啉。通过不同的途径实现2-ABA中存在的两个氨基所需的官能化,这些途径涉及选择性的N-酰化和碳酸铯介导的N-烷基化反应,从而避免了保护/脱保护步骤。通过微波辅助聚磷酸乙酯(PPE)促进的相应氨基酰胺的闭环,可在短反应时间内有效合成杂环。