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1,3-二甲基胸腺嘧啶置于乙醇,Sodium Ethanolate,硫脲体系中,化学反应 15.0H,以74%的收率获得产物4-羟基-2-巯基-5-甲基嘧啶
参考文献:Design,Synthesis And Biological Evaluation Of Cycloalkyl Arylpyrimidines (Capys) As Hiv-1 Nnrtis
标题:Design,Synthesis And Biological Evaluation Of Cycloalkyl Arylpyrimidines (Capys) As Hiv-1 Nnrtis
摘要:A Series Of 18 Cycloalkyl Arylpyrimidines (Capys) Were Designed From Lead Compounds Diarylpyrimidines (Dapys),Synthesized And Evaluated For In Vitro Anti-Hiv Activity. Among Them,The Compound 1P Displayed Potent Anti-Hiv-1 Activity Against Wt Hiv-1 With An Ec50 Value Of 0.055 Mu M And A Selectivity Index (Si) > 7290. The Preliminary Structure-Activity Relationship (Sar) Of This New Series Of Compounds Was Also Investigated,Which Enriched The Sar Of Diarylpyrimidines (Dapys). (C) 2011 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2011.10.002

专利信息

专利号:US-12188072-B2
优先权日:2018-03-19
标题 :Compositions and methods for rapid in vitro synthesis of bioconjugate vaccines in vitro via production and N-glycosylation of protein carriers in detoxified prokaryotic cell lysates
发明人：JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN
权利人:UNIV NORTHWESTERN; UNIV CORNELL
摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated carrier proteins. The glycosylated carrier proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated carrier proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated carrier proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.

专利号:US-12365930-B2
优先权日:2016-07-14
标题:Method for rapid in vitro synthesis of glycoproteins via recombinant production of N-glycosylated proteins in prokaryotic cell lysates
发明人：JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN
权利人:UNIV NORTHWESTERN; UNIV CORNELL
摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated proteins. The glycosylated proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.

专利号:US-2024287520-A1
优先权日:2021-06-30
标题:Method for synthesis of linkage modified oligomeric compounds
发明人：RODRIGUEZ ANDREW A
权利人:IONIS PHARMACEUTICALS INC
摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.

专利号:US-2004152905-A1
优先权日:2003-01-31
标题:Universal building blocks and support media for synthesis of oligonucleotides and their analogs
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and chemically modified oligonucleotide analogs, are provided. In addition, methods for functionalization of a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2024092821-A1
优先权日:2020-03-31
标题:Synthesis of oligonucleotides and related compounds
发明人：ZHONG MINGHONG; JIN YI; GALA DINESH; PRHAVC MARIJA
权利人:JANSSEN BIOPHARMA INC
摘要:Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.