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

Abstract

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 S_NAr substitution, reduction, cyclization, oxidation and tautomerization. The corresponding target products (26 examples) are obtained in 50–90% yield.

Key words

copper - 2-halobenzimidamides - sodium azide - catalysis - 4-aminoquinazolines

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