Ligand‐Controlled Palladium‐Catalyzed Pyridylation of 1‐tert‐Butoxycarbonyl‐3‐iodoazetidine: Regioselective Synthesis of 2‐ and 3‐Heteroarylazetidines

The first efficient regioselective pyridylation of 1‐tert‐butoxycarbonyl‐3‐iodoazetidine to produce 2‐ and 3‐heteroarylazetidines under palladium‐catalyzed conditions has been developed. The established direct pyridylation of azetidines affords 2‐ vs. 3‐heteroarylazetidines in moderate to good yields (up to 92%) and with good regioselectivity (up to 98:2) by using different ligands.