Direct diphosphonylation of quinolines with H-phosphonates under metal-free conditions

Add time:08/12/2019    Source:sciencedirect.com

The ‘one pot’ synthesis of 2,4-diphosphono-1,2,3,4-tetrahydroquinolines starting from quinolines and H-phosphonates has been developed. This transformation involves continuous twice hydrophosphonylation regioselectively and breaks up the aromatic stabilization, which features a simple system, high efficiency, environmental friendliness, under the additives and metal-free conditions. Various of 2,4-diphosphono-1,2,3,4-tetrahydroquinolines were provided in up to 95% yield for 20 examples.

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