2', 3'-DIDEOXY-4-THIO-URIDINE DERIVATIVE, PRODUCTION THEREOF AND ANTIVIRAL AGENT USING SAID DERIVATIVE

摘要

NEW MATERIAL:A derivative shown by formula I (R is H or protecting group such as acetyl or benzoyl). EXAMPLE:2',3'-Dideoxy-4-thio-uridine. USE:An antiviral agent against AIDS, etc. PREPARATION:Hydroxyl groups at 1 and 5'-position of 2',3'-dideoxyuridine as a raw material are protected with a protecting group such as acetyl or benzoyl to give a 2',3'-dideoxyuridine derivative, which is treated with phosphorus pentasulfide (the amount of phosphorus pentasulfide is preferably 1-2mol. based on 1mol. of the compound shown by formula II) in the presence of water in pyridine for 2-5hr, the pyridine solution is concentrated to dryness, the resultant substance is extracted with chloroform and separated to give the aimed substance. The protecting group can be simply removed with an alkali or acid.