Lithiation–Electrophilic Substitution of N‐Thiopivaloylazetidine

The fourth protocol: the rarely studied N-thiopivaloyl group plays a crucial role in mediating efficient α lithiation and incorporation of diverse electrophiles onto an azetidine ring; in the presence of chiral ligands, this chemistry also provides the first example of an enantioselective electrophilic substitution on a four-membered ring.