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.