专利号:US-8193384-B2 优先权日:2005-07-29 标 题 :Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds 发明人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF 权利人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF; RHODE ISLAND EDUCATION 摘要:The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.
专利号:EP-0901500-B1 优先权日:1996-05-03 标题:In situ preparation of nucleoside phosphoramidites and their use in synthesis of oligonucleotides 发明人:ZHANG ZHAODA; TANG JIN-YAN 权利人:AVECIA BIOTECHNOLOGY INC 摘要:The invention provides novel bifunctional phosphitylating reagents and their application in in situ preparation of 5'-protected nucleoside phosphoramidites and synthesis of oligonucleotides. Bifunctional phosphitylating reagents according to the invention react quickly with nucleosides under weakly acidic conditions. In addition, the bifunctional phosphitylating reagents according to the invention generate chemoselectively the corresponding nucleoside phosphoramidites in situ, without need to purify the nucleoside phosphoramidites before using them in oligonucleotide synthesis. Finally, the bifunctional phosphitylating reagents according to the invention are relatively stable and easy to handle.
专利号:US-10730904-B2 优先权日:2012-11-14 标 题:Method for liquid-phase synthesis of nucleic acid 发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO 权利人:TAKEDA PHARMACEUTICALS CO 摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in claim 1 ]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
专利号:US-6340749-B1 优先权日:1995-10-06 标题:Preparation of nucleoside phosphoramidites and oligonucleotide synthesis 发明人:ZHANG ZHAODA; TANG JIN-YAN 权利人:AVECIA BIOTECHNOLOGY INC 摘要:The invention provides novel bifunctional phosphitylating reagents and their application in in situ preparation of 5'-protected nucleoside phosphoramidites and synthesis of oligonucleotides. Bifunctional phosphitylating reagents according to the invention react quickly with nucleosides under neutral or weakly basic conditions, without an additional activation step. In addition, the bifunctional phosphitylating reagents according to the invention generate chemoselectively the corresponding nucleoside phosphoramidites in situ, without need to purify the nucleoside phosphoramidites before using them in oligonucleotide synthesis. Finally, the bifunctional phosphitylating reagents according to the invention are relatively stable and easy to handle.
专利号:US-5859233-A 优先权日:1996-02-21 标 题 :Synthons for synthesis of oligonucleotide N3-P5 phosphoramidates 发明人:HIRSCHBEIN BERNARD L; FEARON KAREN L; GRYAZNOV SERGEI M; MCCURDY SARAH N; NELSON JEFFREY S; SCHULTZ RONALD G 权利人:LYNX THERAPEUTICS INC 摘要:The invention provides a method of synthesizing oligonucleotide N3'->P5' phosphoramidates using an amine-exchange reaction of phosphoramidites in which a -deprotected 3'-amino group of a solid phase supported oligonucleotide chain is exhanged for the amino portion of a 5'-phosphoramidite of an incoming monomer which has a protected 3'-amino group. The resulting internucleotide phosphoramidite linkage is then oxidized to form a stable protected phosphoramidate linkage. The method of the invention greatly improves product yields and reduces reagent usage over currently available methods for synthesizing the above class of compound.
专利号:WO-9742208-A1 优先权日:1996-05-03 标题 :In situ preparation of nucleoside phosphoramidites and their use in synthesis of oligonucleotides
参考标题:Total Synthesis Of The Congested, Bisphosphorylated Morganella Morganii Zwitterionic Trisaccharide Repeating Unit 作者:D. Jamin Keith,Steven D. Townsend |发布日期:2019.8.14 摘要:Zwitterionic Polysaccharides (Zps) Activate T-Cell-Dependent Immune Responses By Major Histocompatibility Complex Class Ii Presentation. Herein, We Report The First Synthesis Of A Morganella Morganii Zps Repeating Unit As An Enabling Tool In The Synthesis Of Novel Zps Materials. The Repeating Unit Incorporates A 1,2-Cis--Glycosidic Bond; The Problematic 1,2-Trans-Galactosidic Bond, Gal-β(1->3)-Galnac;
合成参考文献
摘要:Stankevič, M.; Pietrusiewicz, K. M., Science of Synthesis, (2009) 42, 310.