C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/06 (2006.01) C07H 19/04 (2006.01)
Patent
CA 2439836
The present invention is an efficient synthetic route to 2',3'-dideoxy-2',3'- didehydro-nucleosides from available precursors with the option of introducing functionality as needed, such as, the 2',3'-dideoxy and 2'- or 3'-deoxyribo- nucleoside analogs as well as additional derivatives obtained by subsequent functional group manipulations. Briefly, the present invention discloses a method for the preparation of .beta.-D and .beta.-L-2',3'-dideoxy-2',3'- didehydro-nucleosides starting from appropriately substituted ribonucleosides in two, optionally three steps: Step (1) a haloacylation, such as haloacetylation, and in particular, bromoacetylation; Step (2) a reductive elimination; and optionally, Step (3) a deprotection. The haloacylation of step (1) can form the 2'-acyl-3'-halonucleoside, the 3'-acyl-2'- halonucleoside, or a mixture thereof.
La présente invention concerne un procédé de synthèse efficace de 2',3'-dideoxy-2',3'-didehydro-nucléosides à partir de précurseurs disponibles avec possibilité d'introduire une fonctionnalité selon besoin, tels que les analogues 2',3'-dideoxy et 2'- or 3'-deoxyribo-nucleosides ainsi que des dérivés supplémentaires obtenus par des manipulations de groupe fonctionnel ultérieures. En résumé, cette invention concerne un procédé d'obtention de .beta.-D et .beta.-L-2',3'-dideoxy-2',3'-didehydro-nucleosides en partant de ribonucléosides appropriés, ceci en deux, éventuellement trois opérations: opération (1) halo-acylation, par exemple halo-acétylation, et, en particulier, bromo-acétylation; opération (2) élimination par réduction; et, éventuellement, opération (3) - déprotection. L'opération (1) d'halo-acylation permet d'obtenir le 2'-acyl-3'-halonucléoside, le 3'-acyl-2'-halonucléoside, ou un mélange de ces composés.
Confalone Pasquale N.
Jin Fuqiang
Mbm Intellectual Property Law Llp
Pharmasset Inc.
Pharmasset Ltd.
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