NOVEL 5'-O-ACYLNUCLEOSIDE DERIVATIVE AND ITS PREPARATION

摘要

NEW MATERIAL:A compound expressed formulaI(A is an acyl group of an aminocarboxylic acid, and the N atom of the amino group is acylated by an acyl group of an aliphatic carboxylic acid having one or more groups selected from hydroxy and alkoxyl groups as substituent groups; Z and Z' are H or OH, however, not OH at the same time). EXAMPLE:5'-O-[N-(2,3-Dihydroxypropoxyacetyl)-alanyl]-5-fluorouridine. USE:An antimalignant tumor agent, antiviral agent, immunological inhibitor or an intermediate therefor. PROCESS:The amino group of a nucleoside derivative expressed by formula II (A' is an acyl group of an aminocarboxylic acid) is acylated with a hydroxy- or alkoxyl group-substituted aliphatic carboxylic acid (derivative) to give the compound expressed by formulaI. The compound expressed by formula II is a novel substance, and can be prepared by linking a nucleoside expressed by formula III with an aminocarboxylic acid in which the N-position is protected at the 5'-position.