C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 15/04 (2006.01) C07H 19/06 (2006.01)
Patent
CA 2442979
The present invention is directed to the process for the preparation of 2'- deoxy-2'- halo-.beta.-L-arabinofuranosyl nucleosides of formula (I), and in particular, 2'-deoxy-2'- fluoro-.beta.-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions. (see formula I) wherein X is a halogen (F, Cl, Br or I); and B is a pyrimidine, purine, heterocyclic or heteroaromatic base.
L'invention se rapporte à un procédé de préparation de 2'-deoxy-2'-halo- beta -L-arabinofuranosyl nucléosides, et plus particulièrement de 2'-deoxy-2'-fluoro- beta -L-arabinofuranosyl thymine (L-FMAU), à partir de L-arabinose qui est disponible sur le marché et moins cher que L-ribose ou L-xylose, en 10 étapes. Chacun des réactifs et des produits de base sont bon marché et ne nécessitent pas d'équipement spécial afin de réaliser ces réactions.
Bukwang Pharmaceutical Co. Ltd.
Mbm Intellectual Property Law Llp
Triangle Pharmaceuticals Inc.
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