Domino Knoevenagel Condensation/Intramolecular Aldol Cyclization Route to Diverse Indolizines with Densely Functionalized Pyridine Units

A highly efficient [4 + 2] annulation route to polysubstituted indolizines is described employing a domino Knoevenagel condensation/intramolecular aldol cyclization process as a key step. Construction of pyridine rings in indolizine skeleton was rapidly achieved from several pyrrole-2-carboxaldehydes in good to excellent yields, leading to indolizines with various substituents at the 5, 6, and 7 positions depending on the reacting active methylene partners

Palladium-Catalyzed α‑Arylation of Aryloxyketones for the Synthesis of 2,3-Disubstituted Benzofurans

A highly efficient palladium-catalyzed α-arylation of aryloxyketones has been developed, allowing for facile installation of various (hetero)­aryl groups at C2 position in good to excellent yields. Subsequent cyclodehydration of the resulting α-arylated aryloxyketones provided rapid access to diverse 2,3-disubstitured benzofurans