Synthesis of Indolines and Tetrahydroisoquinolines from Arylethylamines by Pd^II‐Catalyzed CH Activation Reactions

Abstract

Hand in hand: A versatile CH activation route for the synthesis of indolines, tetrahydroquinolines, and tetrahydroisoquinolines from simple arylethylamines relies on a one-pot iodination and amination reaction (see scheme, Tf=trifluoromethanesulfonyl). The natural amino acids phenylalanine, tyrosine, and tryptophan can be converted into various heterocycles by using this technology.