Direct arylation of azine N-oxides with aryl triflates

作者：Schipper Derek J; El Salfiti Mohamed; Whipp Christopher J; Fagnou Keith^*

来源：Tetrahedron, 2009, 65(26): 4977-4983.

DOI：10.1016/j.tet.2009.03.077

Palladium catalyzed direct arylation of azine N-oxides using aryl triflates to afford the corresponding 2-aryl azine N-oxides is described. The reaction is carried out with a range of both N-oxides and aryl triflates. The arylation can be carried out in sequence to yield differentially diarylated products. The regioselectivity and scope of 3-substituted azine N-oxides are investigated. The method is applied to the synthesis of a compound that exhibits antimalarial and antimicrobial activities.

• 出版日期2009-6-27