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

摘要

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 hydro-phosphonylation 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. (C) 2015 Elsevier Ltd. All rights reserved.