5-methyluridine process for large-scale preparation of 2',3'-didehydro-3'-deoxythymidine (d4T)

摘要

An economical process, amenable to large-scale production, is disclosed for the preparation of 2',3'-didehydro-3'-deoxythymidine (d4T) from 5-methyluridine. The process employs a novel, 5'-benzoyl-2' alpha -halo-3' alpha -alkanesulfonylthymidine intermediate as well as a highly efficient and practical deprotection, isolation and purification procedure for the d4T product.