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- W2011017095 abstract "Coupling of 6-benzyl-5-hydroxymethyluracil (1) with formaldehyde acetals followed by fluorination using (diethylamino)sulfur trifluoride (DAST) afforded 1-alkenyloxymethyl and 1-propargyloxymethyl 5-fluoromethyl-6-benzyluracils 3a-c. 6-(3,5-Dimethylbenzyl)-5-ethyl-1-[(2-fluoroethoxy)methyl]pyrimidine-2,4(1H,3H)-dione (6) was synthesized by fluorination of the corresponding hydroxy derivative 5. Sonogoshira reaction was performed on 6-(3,5-dimethylbenzyl)-5-ethyl-1-(4-iodobenzyl)uracil (7) with propargyl alcohol to afford 8 which was fluorinated to give the fluoro propargyl derivative 9. Compound 7 was synthesized by N1-alkylation of the corresponding uracil. Significant activity was found against HIV-1 except for compounds with 5-hydroxymethyl and 5-fluoromethyl substituents." @default.
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- W2011017095 date "2011-04-01" @default.
- W2011017095 modified "2023-09-24" @default.
- W2011017095 title "Synthesis and Anti-HIV-1 Activity of New Fluoro-HEPT Analogues: An Investigation on Fluoro versus Hydroxy Substituents" @default.
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- W2011017095 doi "https://doi.org/10.1002/ardp.201000187" @default.
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