Ru(II)‐Catalyzed Weak Chelation‐Assisted Regioselective C4−H Aminomethyl Alkenylation of Indole

Abstract A Ruthenium catalyzed C4‐ aminomethyl alkenylation of indoles using substituted propargylamine as an alkenylating agent and pivaloyl as a weak chelating group has been demonstrated. A variety of substituted indoles and propargylamines furnished the desired product in good yields. Control experiments indicate that the C−H cleavage step is reversible and suggest the possibility of a base‐assisted internal electrophilic substitution (BIES) pathway.