The Pd-catalyzed copper-free carbonylative Sonogashira coupling reaction to synthesize alkynyl ketones from terminal alkynes and aryl iodides was achieved by using water as a solvent. The reaction was carried out at room temperature under balloon pressure of CO with Et(3)N as a base. The developed method was successfully applied to the synthesis of flavones.

A one-pot synthesis of diverse benzofurans and indoles from readily available starting materials was achieved via the sequential Ugi four-component reaction, intramolecular Diels-Alder reaction, and oxidative aromatization.

A novel C 2 symmetrical and sterically bulky thiourea ligand 1 has been successfully applied to Heck, Suzuki and Suzuki-type carbonylative coupling reactions under aerobic conditions. Since the metal-sulfur bond in the thiourea complexes is stronger than the metal-phosphorus bond of typical phosphine complexes, thiourea ligands generally do not easily dissociate from the metal center under catalytic conditions, which establishes the thiourea 1-based palladium complexes as effective catalysts for the palladium-catalyzed cross-coupling reactions.

Ketones Q 0350Pd-Catalyzed Copper-Free Carbonylative Sonogashira Reaction of Aryl Iodides with Alkynes for the Synthesis of Alkynyl Ketones and Flavones by Using Water as a Solvent. -(LIANG, B.; HUANG, M.; YOU, Z.; XIONG, Z.; LU, K.; FATHI, R.; CHEN*, J.; YANG, Z.; J. Org. Chem. 70 (2005) 15, 6097-6100; Key Lab. Bioorg.

A multi-component one-pot protocol for efficient preparation of various heterocyclic compounds is developed. The method is expected to find valuable applications in combinatorial chemistry, diversity-oriented synthesis and drug discovery. -(LU, K.; LUO, T.; XIANG, Z.; YOU, Z.; FATHI, R.; CHEN, J.; YANG*, Z.; J. Comb. Chem. 7 (2005) 6, 958-967; Lab. Chem. Gen., Shenzhen Grad. Sch., Peking Univ., Beijing 100871, Peop. Rep. China; Eng.) -Nuesgen 15-107