Synthesis p. 2535 - 2535 (2017)
Update date:2022-08-02
Topics:
Yang, Lei
Luo, Honghua
Sun, Yan
Shi, Zhenyu
Ni, Kaidong
Li, Fei
Chen, Dongyin
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.
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