Synthesis and investigation of antiviral activity of 3′-O-(aminoalkyl)-thymidines and their quaternary ammonium salts

摘要

Alkylation of 5′-O-tritylthymidine with dialkylaminoalkyl chlorides in the presence of sodium hydride yields 3′-O-dialkylaminoalkyl-5′-O-tritylthymidine derivatives2which were treated with an excess of iodomethane to afford the corresponding quaternary ammonium derivatives3. Deprotected nucleosides4and6were obtained by refluxing3and2, respectively, in 80 acetic acid. When the compounds2–4and6were investigated for activity against HSV and HIV, the trityl derivatives2aand2cwere found active agai