PROCESS FOR THE PRODUCTION OF ANTIVIRAL PREPARATIONS CONTAINING 6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS ACTIVE AGENTS AND PROCESS FOR THE PRODUCTION OF THE ACTIVE AGENTS

摘要

A 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I min ; CHEM wherein R1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group; R2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a haloger atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups; R3 represents a hydrogen atom, methyl, branched alkyl or -CH2-Z-(CH2)n-R5 group where R5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5, R4 represents a hydrogen atom, alkyl or aralkyl group, X represents an oxygen or sulfur atom, Y represents an oxygen or sulfur atom, provided that when R4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R5 does not represent a hydroxyl group, or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient.