3-Phosphinoylindole derivatives play important roles as pharmaceutical drugs and ligands. A new method for the synthesis of 3-phosphinoylindole derivatives has been achieved through silver-mediated cycloaddition between N-Ts-2-alkynylaniline derivatives and H-phosphine oxides. This transformation offers a straightforward route to the formation of the C-P bond, indole ring, and desulfonylation in one step.
The reaction of P4 with arylthiols in the presence of Na2–eosin Y under visible light gave phosphorotrithioites. Subsequent oxidation of phosphorotrithioites produced phosphorotrithioates. The phosphorotrithioate 3f presents good inflammation reducing characteristics.
The first Pd-catalyzed domino Heck/ phosphorylation of N-(2-iodophenyl)acrylamides with secondary phosphine oxides has been developed. The use of PdCl 2 as a catalyst, 1,4-bis (diphenylphosphino)butane as a ligand, K 2 CO 3 as a base, various N-(2-iodophenyl)acrylamide derivatives are tolerant in this transformation, affording 3phosphinomethyl 3,3-disubstituted oxindole products in good to excellent yields. This transformation offers a straightforward route to the formation of the new CÀ C and PÀ C bonds, oxindole ring in one step. Moreover, this method can be easily adapted to large-scale preparation. Scheme 1. The route to oxindole-based phosphine oxides.
The first general and high-yielding synthesis of mixed phosphorotrithioates (R1S)2P(O)SR2 involving white phosphorus, disulfides, and alkyl halides is presented, which opens the shortest and environmentally benign way to these compounds...
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