PROCESS FOR LARGE-SCALE SYNTHESIS OF 2', 3'-DIDEHYDRO-3'-DEOXYTHYMIDINE (D4T) INVOLVING THE ISOLATION OF A D4T N-METHYLPYRROLIDINONE SOLVATE AND THE INTERMEDIATE D4T NMPO SOLVATE THEREFOR

摘要

An improved process suitable for large-scale production of 2',3'-didehydro-3'-deoxythymidine (d4T) and close analogs is disclosed. The improved process yields d4T in high yield and purity without the use of hazardous reactions or reagents and incorporates several process improvements important on a large scale including a novel purification step involving the isolation of a d4T.N-methylpyrrolidinone solvate.