IMPROVED PROCESS FOR THE SYNTHESIS OF 2'-O-SUBSTITUTED PYRIMIDINES AND OLIGOMERIC COMPOUNDS THEREFROM
摘要
<p>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.</p>
申请公布号
EP0813539(A1)
申请公布日期
1997.12.29
申请号
EP19960910385
申请日期
1996.03.06
申请人
ISIS PHARMACEUTICALS, INC. ISIS PHARMACEUTICALS, INC.
发明人
COOK, PHILLIP, DAN;SANGHVI, YOGESH, S.;SPRANKLE, KELLY G.;ROSS, BRUCE, S.;GRIFFEY, RICH, H.;SPRINGER, ROBERT, H.
