Metal-Free One-Pot Three-Component Synthesis of Quinazoline Derivatives via Peroxide-Mediated Direct Oxidative Amination of C(sp3 )-H Bonds

摘要

An efficient, one-pot synthesis of 4-substituted quinazoline derivatives via direct oxidative amination of C(sp3 )-H bonds was demonstrated. The nature of the oxidant exhibited a considerable effect on the reaction, and tert-butyl hydroper- oxide in decane emerged as the best option. A variety of C1 sources could be used, affording 4-substituted quinazolines in good yields. The three-component reaction proceeded readily without any added catalyst, in which acetic acid from ammonium acetate was essential for the catalytic cycle. This protocol would offer a complementary pathway to previous methods in the synthesis of 4-substituted quinazoline deriva- tives.