5-methyluridine process for large-scale preparation of...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/073 (2006.01) C07H 19/06 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2135852

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.

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