尿嘧啶置于硫酸 双氧水,碘,乙酸酐,尿素体系中,用 溶剂黄146 作为反应溶剂,以25%的收率获得产物5-碘尿嘧啶 参考文献:Eco-Friendly Oxidative Iodination Of Various Arenes With A Urea-Hydrogen Peroxide Adduct (Uhp) As The Oxidant 标题:Eco-Friendly Oxidative Iodination Of Various Arenes With A Urea-Hydrogen Peroxide Adduct (Uhp) As The Oxidant 摘要:本文介绍了三种简便的环保实验室流程,利用稳定的,强氢键结合的固体尿素-过氧化氢加合物uhp(过碳酰胺)作为氧化剂,在分子碘的存在下,对各种活化和非活化芳烃进行氧化碘化反应. DOI:10.1055/s-2004-815955
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-8618279-B2 优先权日:2009-01-15 标 题 :Synthesis of 2′,3′— and 3′,5′—cyclic phosphate mono-and oligonucleotides 发明人:LAIKHTER ANDREI; SRIVASTAVA SURESH CHANDRA; SRIVASTAVA NAVEEN 权利人:LAIKHTER ANDREI; SRIVASTAVA SURESH CHANDRA; SRIVASTAVA NAVEEN; CHEMGENES CORP 摘要:The invention provides a novel method for the chemical synthesis of 2′,3′-cyclic phosphate and phosphorothioate of mono and terminated oligonucleotides synthesis. The invention also provides a novel method of for the chemical synthesis of 2′,3′- and 3′,5′-cyclic phosphate and phosphorothioate mononucleotide nucleotides. The process is based on quick and efficient cyclization of phosphoramidate moiety and neighboring hydroxyl group. The present invention is directed towards the synthesis of high purity DNA and RNAs, specifically to introduce cyclic phosphate at 3′-end of oligonucleotides. Such DNA and RNA's have extensive application in therapeutics, diagnostics, drug design, and selective inhibition of an RNA sequence within cellular environment, in pre-tRNA cleavage and in ribozyme ligation. The 2′,3′-cyclic phosphate nucleosides are involved in a vast number of applications in molecular biology in general and mammalian cells in particular. The invention also envisions providing kits comprising at least one composition disclosed in the present invention.
专利号:US-5977301-A 优先权日:1992-09-24 标题 :Synthesis of N-substituted oligomers 发明人:ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
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:EP-0671928-B1 优先权日:1992-09-24 标题 :Synthesis of n-substituted oligomers 发明人:ZUCKERMANN RONALD N; KERR JANICE M; KENT STEPHEN BRIAN HENRY; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R<9>) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using the automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:US-5789577-A 优先权日:1994-12-30 标 题 :Method for the controlled synthesis of polynucleotide mixtures which encode desired mixtures of peptides 发明人:GEYSEN H MARIO 权利人:CHIRON CORP 摘要:A method to obtain selected individual polynucleotides or mixtures thereof each of which encodes a peptide and at least one polynucleotide of the mixture encodes a peptide having a target property. The polynucleotides of the invention present in the mixture in detectable, retrievable, and clonable amounts are expressed in a host organism for screening for the target activity. The invention features the ability to synthesize controlled random polynucleotides to produce a predetermined mixture of polynucleotides and to avoid synthesis of a stop codon by adjusting the proportions into which the synthesis pool is subdivided and by adjusting the proportions of activated nucleotides added at each coupling step. A polynucleotide encoding a peptide having a target property can be selected and sequenced to deduce the amino acid sequence of the peptide.
参考标题:The [2+2] Photocycloaddition Of Uracil Derivatives With Ethylene As A General Route To Cis-Cyclobutane β-Amino Acids 作者:David Aitken,Christine Gauzy,Bertrand Saby,Elisabeth Pereira,Sophie Faure |发布日期:2006.6 摘要:A Three-Step Procedure, Based On The [2+2]-Photochemical Reaction Of Uracils With Ethylene Followed By Controlled Degradation Of The Heterocyclic Ring, Has Been Developed For The Synthesis Of A Range Of C1- And C2-Substituted Cis-Cyclobutane î²-Amino Acids, In Good Overall Yield.
合成参考文献
摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 66. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 349. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 371. 摘要:Yorimitsu, H.; Oshima, K., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 652. 摘要:Chanda, A.; Fokin, V. V., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 737.