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|Title:||Arylation of 2-Furyl 4-Fluorophenyl Ketone: an extension of Heck Chemistry towards Novel Integrase Inhibitors||Authors:||Franchi, Luigi
|Keywords:||Heck reaction; direct arylation; 2-acylfurans; catalysis; integrase inhibitors||Issue Date:||2010||Project:||None||Journal:||SYNTHESIS||Abstract:||
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.
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