A Highly Efficient Copper-Catalyzed Three-Component Synthesis of 4-Aminoquinazolines

作者:Yang, Lei; Luo, Honghua; Sun, Yan; Shi, Zhenyu; Ni, Kaidong; Li, Fei; Chen, Dongyin*
来源:Synthesis (Germany), 2017, 49(11): 2535-2543.
DOI:10.1055/s-0036-1588727

摘要

A highly efficient copper-catalyzed one-pot protocol is developed for the synthesis of 4-aminoquinazolines from easily available 2-iodo- or 2-bromobenzimidamides, aldehydes, and sodium azide. This one-pot approach proceeds via consecutive copper-catalyzed SNAr substitution, reduction, cyclization, oxidation and tautomerization. The corresponding target products (26 examples) are obtained in 50-90% yield.