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Title: Arylation of 2-Furyl 4-Fluorophenyl Ketone: an extension of Heck Chemistry towards Novel Integrase Inhibitors
Authors: Franchi, Luigi
Rinaldi, Marta
Vignaroli, Giulia
Innitzer, Anna
Radi, Marco
Botta, Maurizio 
Keywords: Heck reaction; direct arylation; 2-acylfurans; catalysis; integrase inhibitors
Issue Date: 2010
Project: None 
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.
ISSN: 0039-7881
DOI: 10.1055/s-0030-1258247
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