Synthesis of d4T-5'-glycosyl-1'-phosphoramidates from H-phosphonates via an oxidative coupling strategy

摘要

An improved synthetic method based on glycosyl-1″-H-phosphonate diesters has been developed for the preparation of O-d4T-5' -O-glycosyl-1″-phosphoramidate diesters, a kind of potential anti-HIV prodrugs. The target products were synthesized in high yields by using the CCl_4/Et_3N/amino acid methyl ester system.