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Synthons for oligonucleotide synthesis

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专利名称:Synthons for oligonucleotide synthesis发明人:Radhakrishnan P. Iyer,Dong Yu,Mao-Jun

Guo,Sudhir Agrawal

申请号:US09/015472申请日:19980129公开号:US06117993A公开日:20000912

摘要:The invention provides new reagents and processes for synthesizing

oligonucleotides, including stereoselective oligonucleotide synthesis. In a first aspect, theinvention provides novel monomer synthons for the synthesis of oligonucleotides.Monomer synthons according to this aspect of the invention are useful in the synthesis ofoligonucleotides and can be used in place of the well known beta- cyanoethyl

phosphoramidite monomer synthon in the phosphoramidite synthesis procedure. Certainmonomer synthons according to this aspect of the invention are useful in this procedurefor producing oligonucleotides having defined stereochemistry.

In a second aspect, the invention provides processes for synthesizing monomersynthons according to the invention, including diastereomerically enriched or purifiedmonomer synthons. In the processes according to this aspect of the invention, thechemical reactions are stereoretentive so that the products of each reaction retain thesame stereoconfiguration as their precursor reagent.

In a third aspect, the invention provides processes for synthesizing oligonucleotidesusing the well known phosphoramidite approach. In the processes according to thisaspect of the invention, any of the monomer synthons according to the invention is used

in place of the conventional beta-cyanoethyl phosphoramidite.

申请人:HYBRIDON, INC.

代理机构:McDonnell Boehnen Hulbert & Berghoff

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