Arylation of 2-Furyl 4-Fluorophenyl Ketone: An Extension of Heck Chemistry towards Novel Integrase Inhibitors

An optimized procedure for the direct and regioselective arylationof 2-acylfurans has been developed. The versatility of this protocolhas been evaluated on a series of aryl and heteroaryl halides, thusobtaining a small collection of 2,5-disubstituted furans in moderateto good yields. Finally, the optimized protocol has been successfullyapplied to the synthesis of the HIV-1 integrase inhibitor 3 and could be further exploited for thegeneration of novel substituted furans as potential integrase inhibitors.