Process for preparing AZT and derivatives thereof

摘要

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.