SULFUR DERIVATIVES OF 2'-FLUORO-5-METHYL-BETA-L-ARABINO FURANOSYL URIDINE AND PREPARATION PROCESS THEREOF

摘要

PURPOSE: Sulfur derivatives of 2'-fluoro-5-methyl-beta-L-arabino furanosyl uridine and a preparation process thereof are provided, which compounds have antiviral activity, especially anti-Hepatitis B virus(HBV) activity and less nerve toxicity. CONSTITUTION: The sulfur derivatives of 2'-fluoro-5-methyl-beta-L-arabino furanosyl uridine include 1 - (3 - fluoro - hydroxy - 5 - mercaptomethyl - tetrahydro - furan - 2 - il) - 5 - methyl - 1H - pyrimidine - 2,4 - dion represented by formula(1) and 1 - (3 - fluoro - hydroxy - 5 - (methyl - oxomethylene - 14 - sulfanylmethyl) - tetrahydro - furan - 2 - il) - 5 - methyl - 1H - pyrimidine - 2,4 - dion represented by formula 2. The process for preparing the compound of formula(2) comprises reacting L-FMAU compound represented by formula(3) with trialkylphosphin, dialkylazodicarboxylate and thiolacetate in a solvent selected from THF, benzene, diethylether, dioxane, HMPT, pyridine and N,N-dimethylformamide at -10 deg. C to the room temperature.