Abstract

An experimentally simple and convenient synthesis of 4-susbstituted 2-(trichloromethyl)quinazolines by cycloaddition of benzyne with 2-(trichloromethyl)-1,3-diazabutadienes was developed. The 2-(trichloromethyl)-1,3-diazabutadienes (R1 = H and Me) were prepared from trichloroacetamidine and the appropriate N,N-dimethylamide dimethyl acetal or from trichloroacetamidine and a Vilsmeier–Haack reagent containing an aryl group.

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