Abstract

An efficient direct amination of quinazolin-4(3<i>H</i>)-ones using <i>N</i>,<i>N</i>-dimethylformamide as a nitrogen source is described that affords the corresponding 4-(dimethylamino)quinazolines in high yields. This transformation proceeds through efficient 4-toluenesulfonyl chloride mediated C–OH bond activation at room temperature.

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