Process for preparing AZT
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United States of America Patent
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Nov 14, 1995
Grant Date -
N/A
app pub date -
Nov 15, 1993
filing date -
Nov 15, 1993
priority date (Note) -
Expired
status (Latency Note)
Importance
Abstract
A process for preparing AZT and comprising the steps of: a) reacting a 2'-halo-5'-protected pyrimidinyl 2'-deoxyribonucleoside having a 3'-sulfonyl group with tributyl tin hydride and catalytic amount of azobisisobutyronitrile in an ether, ester, or ketone solvent to yield a dehalogenated pyrimidinyl 2'-deoxyribonucleoside; followed by b) reacting said dehalogentated pyrimidinyl 2'-deoxynucleoside formed in step (a) with a base, a lithium salt, and an azide salt to yield a 5'-protected pyrimidinyl 3'-dideoxy-3'-azido-ribonucleoside; and c) deprotecting the nucleoside derivative of step (b) to yield 3'-dideoxy-3'-azidothymidine.
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