Process for preparing azt and derivatives thereof

C - Chemistry – Metallurgy – 07 – H

Patent

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

Patent

CA 2135854

ABSTRACT PROCESS FOR PREPARING AZT AND DERIVATIVES THEREOF Disclosed is a process for producing AZT (3'-azido-3'- deoxythymidine) and derivatives thereof. The process makes use of a reduction step wherein a 2'-halo-5'-protected pyrimidinyl 2'-deoxyribonucleoside compound is reduced in an ether, ester, or ketone solvent. Also, the process makes use of a displacement step wherein a 3'.alpha.-sulfonyl group is displaced with an azido group in the presence of a lithium salt and a base.

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