One-Step Palladium-Catalyzed Heterocyclic Ring Closure of Benzofurans with Aryl Iodides through a Heck-Type Pathway.

An operationally simple and robust method for the direct arylation and ring closure of benzofurans is reported. Besides the mild conditions and good reaction yields, the methodology is applicable for a wide range of derivatives using commercially available aryl iodides with complete C regioselectivity. The reaction is proposed to follow a Heck-type oxyarylation mechanism.

1,3-Diamine-Derived Catalysts: Design, Synthesis, and the Use in Enantioselective Mannich Reactions of Ketones.

1,3-Diamine-derived catalysts were designed, synthesized, and used in asymmetric Mannich reactions of ketones. The reactions catalyzed by one of the 1,3-diamine derivatives in the presence of acids afforded the Mannich products with high enantioselectivities under mild conditions. In most cases, bond formation occurred at the less-substituted α-position of the ketone carbonyl group.