NUCLEOSIDE-5'-O-MORPHOLINOACYL ESTER AND ITS PREPARATION

摘要

NEW MATERIAL:A nucleoside-5'-O-morpholinoacyl ester expressed by formulaI (A is an acyl group of a saturated fatty acid having a morpholino group at the alpha- or omega-position; Z and Z' are H or OH, however not OH at the same time). EXAMPLE:5'-O-(5-Morpholinopentanoyl)-5-fluorouidine. USE:An antimalignant tumor agent, antiviral agent and immunological inhibitor. PROCESS:A saturated fatty acid having a morpholino group at the alpha- or the omega- position is esterified with a nucleoside expressed by formula II e.g. 5-fluorouridine, in an anhydrous solvent, e.g. benzene or chloroform, in the presence of a basic compound, e.g. a trialkylamine or pyridine, and a condensing agent, e.g. p-toluenesulfonyl chloride, at 40 deg.C or below to form an ester bond and give the compound expressed by formulaI.