Synthesis and anti-HIV Activity of C4-Modified Pyrimidine Nucleosides.

Abstract One-pot syntheses provided a series of triazole- and pentafluorophenyloxy-substituted pyrimidine nucleosides. Most of the compounds in the series displayed anti-HIV activities but none as potent as AZT 2 . 1-(β- d - Erythro -pentofuranosyl)-4-pentafluorophenyloxy-2(1 H )-pyrimidinone 14 was the most potent and the most selective compound in the series with EC 50 =1.6 μM.