ChemInform Abstract: Palladium‐Catalyzed Intramolecular Cyclization of Ynamides: Synthesis of 4‐Halo‐oxazolones.

• DOI: 10.1002/chin.201532148
• Publication Date: 2015-07-24T09:14:10Z
• Authors: Hai Huang; Guangke He; Guohao Zhu; Xiaolin Zhu; Shineng Qiu; Hongjun Zhu
• Keywords: Halogens; Molecular Structure; Cyclization; Oxazolone; 01 natural sciences; Catalysis; Copper; Palladium; 0104 chemical sciences

A mild and efficient methodology involving Pd(PPh3)4-catalyzed intramolecular cyclization of N-alkynyl alkyloxycarbamates with CuCl2 or CuBr2 for the synthesis of 4-halo-oxazolones was developed. This reaction exhibiting good functional tolerance provided a new, efficient, and rapid synthetic process to 4-halo-oxazolones. The resulting 4-halo-oxazolones can serve as great potential precursors for the 3,4,5-trisubstituted oxazolones via a Pd-catalyzed cross-coupling reaction.