<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A novel methodology for the asymmetric synthesis of trans‐3, 4‐diaryl‐substituted tetrahydroquinolines via sparteine‐assisted stereoselective lithiation of o‐substituted N‐pivaloylanilines (I), kinetic resolution of epoxides in substitution and a stereospecific Mitsunobu cyclization is developed.</p> </abstract>