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 α- or ω-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 α- or the ω- 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°C or below to form an ester bond and give the compound expressed by formulaI.
SAKAI KATSUMI
CHIYOU KIYOAKI
INAMOTO YOSHITAKA
TESHIGAHARA HARUHIKO
