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|Title:||Process for the synthesis of 2'-O-substituted pyrimidines and oligomeric compounds therefrom|
|Abstract:||Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2' and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position. Improved processes for the synthesis of 2'-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2'-anhydropyrimidine nucleoside or a 2S,2'-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.|
|Inventor(s):||Cook; Phillip Dan (Escondido, CA), Sanghvi; Yogesh S. (Encinitas, CA), Sprankle; Kelly G. (Vista, CA), Ross; Bruce S. (Carlsbad, CA), Griffey; Rich H. (Vista, CA), Springer; Robert H. (Carlsbad, CA)|
|Assignee:||Isis Pharmaceuticals, Inc. (Carlsbad, CA)|
Patent Claim Types:|
see list of patent claims
|PCT Filed||March 06, 1996||PCT Application Number:||PCT/US96/03174|
|PCT Publication Date:||September 12, 1996||PCT Publication Number:||WO96/27606|
|Country||Document Number||Estimated Expiration||Supplementary Protection Certificate||SPC Country||SPC Expiration|
|European Patent Office||0813539||► Subscribe|
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