An optimized procedure for the direct and regioselective arylation of 2-acylfurans has been developed. The versatility of this protocol has been evaluated on a series of aryl and heteroaryl halides, thus obtaining a small collection of 2,5-disubstituted furans in moderate to good yields. Finally, the optimized protocol has been successfully applied to the synthesis of the HIV-1 integrase inhibitor 3 and could be further exploited for the generation of novel substituted furans as potential integrase inhibitors.
Arylation of 2-Furyl 4-Fluorophenyl Ketone: An Extension of Heck Chemistry towards Novel Integrase Inhibitors / Luigi Franchi; Marta Rinaldi; Giulia Vignaroli; Anna Innitzer; Marco Radi; Maurizio Botta. - In: SYNTHESIS. - ISSN 0039-7881. - 2010(2010), pp. 3927-3933. [10.1055/s-0030-1258247]
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