Three-component synthesis of functionalized pyrrolo[3,4-c]quinolin-1-ones by an unusual reductive cascade reaction

We developed the first one-pot synthesis of structurally diverse pyrrolo[3,4-c]quinoline-1-one derivatives via a three-component cascade reaction of enaminones, amines, and isatin under acidic condition. This reaction proceeds through an unusual hydride transfer from in situ formed dimethylamine to a carbocation intermediate to generate the 3-methylene group. This method is straightforward, high-yield, easy to operate, and shows a broad substrate scope, thus potentially useful for diversity-oriented synthesis.

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