1- (CYCLOPENT-3-EN-1-YL)METHYL -5-ETHYL-6-(3,5-DIMETHYLBENZOYL)-2,4- PYRIMIDINEDIONE AND PROCESS FOR PREPARATION THEREOF

摘要

PURPOSE: Provided are preparation method for 1- £(Cyclopent-3-en-1-yl)methyl|-5-ethyl-6-(3,5-dimethylbenzoyl)-2,4-pyrimidinedione and acid addition salts thereof useful as an antiviral agent, in particular, a therapeutic agent of low toxicity for AIDS in high yield using a simple process. CONSTITUTION: The 1-£(Cyclopent-3-en-1-yl)methyl| -5-ethyl-6-(3,5-dimethylbenzoyl)-2,4-pyrimidinedione having high antiviral activity against HIV-1 is prepared by the reaction of a compound of formula (IV) and a compound (III) in the presence of a base at 10 to 100 deg.C for 4 to 72 hrs with oxygen addition. In formula (III), Lie is a departing group such as halogen atom, alkylsulfonyl or arylsulfonyl.