Reliable Synthesis of Phosphino‐ and Phosphine Sulfide‐1,2,3,4‐Tetrahydroquinolines and Phosphine Sulfide Quinolines

The synthesis of phosphino‐ and phosphine sulfide‐1,2,3,4‐tetrahydroquinolines and phosphine sulfide quinolines is described. The synthetic route involves a multicomponent reaction of 2‐phosphinoaniline or 2‐phosphine sulfide‐aniline, aldehydes, and styrenes for the preparation of phosphino‐ or phosphine sulfide‐1,2,3,4‐tetrahydroquinolines and allows for the selective generation of two stereogenic centers in a short, efficient, and reliable approach. The selective oxidation of phosphine sulfide‐1,2,3,4‐tetrahydroquinolines led to the formation of the phosphine sulfide quinolines. A method based on a multicomponent Povarov reaction has been developed for the synthesis of phosphino‐ and phosphine sulfide‐1,2,3,4‐tetrahydroquinolines and phosphine sulfide quinolones. The reactions of phosphino and phosphine sulfide aniline derivatives with aldehydes and styrenes selectively generated two stereogenic centers in a single step with excellent regioselectivity.