| 摘要 |
FIELD: chemistry.SUBSTANCE: present invention relates to a novel (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate of general formula I or a stereoisomer or a pharmaceutically acceptable salt thereof, having properties of nucleoside inihibitors of RNA polymerase NS5B of the hepatitis C virus. The invention also relates to a method of producing compounds, pharmaceutical compositions and a medicinal agent based on said compounds. In general formula 1, Ris hydrogen, (CH)[(CH)C]Si, C-Cacyl, optionally substituted with a benzyloxy group, NRRgroup, wherein Rand Rare independently hydrogen or C-Calkyl; 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl or piperidin-4-ylcarbonyl; Rand Rare F or Ris F or OH and Ris CH; Ris hydrogen or methyl; Ar is phenyl, pyridyl or naphthyl, where the phenyl, pyridyl or naphthyl is optionally substituted with at least one of Calkyl, Calkenyl, Calkynyl, Calkoxy, F, Cl, Br, I, nitro, cyano, -N(Calkyl); Pm is 2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl or 4-(4-amino-2-oxo-2H-pyrimidin-1-yl), wherein the amino group is optionally substituted with 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl, piperidin-4-ylcarbonyl or a C(O)Rradical, where Ris C-Calkyl, optionally substituted with a NRRgroup, where Rand Rare independently hydrogen or C-Calkyl; Calkoxy, optionally substituted with a phenyl; X is O or N-R, where Ris C-Calkyl, optionally substituted with OH or OCH; n=1, 2 or 3.EFFECT: compounds can be used to prevent and treat viral infections, including hepatitis C.12 cl, 1 tbl, 11 ex |
