Abstract
AbstractWe have developed a regioselective hydroarylative coupling of indolines with internal alkynes by the activation of C−H bond using inexpensive Ru(II)‐catalyst. This redox‐neutral, atom‐economical, and scalable C−H functionalization has been accomplished using easily removable weakly coordinating directing group. Diverse unsymmetrically substituted alkynes appended with pharmacologically important heterocycles were coupled with various indolines and 1,2,3,4‐tetrahydroquinolines to furnish the corresponding trisubstituted alkenes with very high regioselectivity. The application of the method has been demonstrated with a number of alkyne‐containing drug molecules, natural products, carbohydrates, amino acids, steroids, and other heterocycles. Preliminary mechanistic interrogation revealed that the C−H activation proceeds through base‐assisted internal electrophilic‐type substitution process.
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