CAS: 51-20-7; 5-Bromopyrimidine-2,4(1H,3H)-Dione

上下游产品

CAS号664988-37-8 5-bromo-2,4-bis... | CAS号66-22-8 尿嘧啶 | CAS号71-30-7 胞嘧啶 | CAS号3252-17-3 sodium isoorotate | CAS号1124-83-0 5,5-Dibromo-5,6... | CAS号56686-16-9 5-溴-2,4-二甲氧基嘧啶 | CAS号36082-50-5 5-溴-2,4-二氯嘧啶 | CAS号7783-56-4 三氟化锑 | CAS号105411-91-4 5-bromo-1-(4-me... | CAS号105411-92-5 5-bromo-1-(4-et... | CAS号105411-94-7 5-bromo-1-(4-bu... | CAS号55476-33-0 5-(2-羟基乙基)氨基尿嘧啶 | CAS号141692-27-5 5-[benzyl(methy... | CAS号206762-91-6 3-benzoyl-5-bro... | CAS号120-89-8 仲班酸 | CAS号102636-37-3 isodialuric acid | CAS号19645-78-4 5-溴嘧啶-2,4,6(1h,... | CAS号3237-50-1 5,5-二羟基六氢嘧啶-2,4,6-三酮

尿嘧啶置于溴体系中,用 水 作为反应溶剂,以96.3%的收率获得产物5-溴尿嘧啶
参考文献:选择性p2Y2受体拮抗剂ar-C118925的合成,表征和体外评估.
标题:选择性p2Y2受体拮抗剂ar-C118925的合成,表征和体外评估.
摘要:对于g Q蛋白偶联,Atp-和utp激活p2Y 2受体是用于一系列不同的疾病,包括肿瘤转移,炎症,动脉粥样硬化,肾脏疾病,和骨质疏松症的潜在药物靶标,但药理学研究由限制阻碍合适的拮抗剂的可用性.最有效和选择性的拮抗剂之一是硫尿嘧啶衍生物ar-C118925.然而,该化合物直到最近才可商购,并且对其性质知之甚少.因此,我们开发了一种改进的合成ar-C118925和两种衍生物的方法,以实现放大生产,并评估了其在人和大鼠p2Y 2的钙动员测定中的功效.受体在1321N1星形细胞瘤细胞中重组表达.进一步评估了该化合物对p2Y 2受体诱导的β-Arrestin移位的抑制作用.ar-C118925表现为p A 2的竞争性拮抗剂值分别为37.2 Nm(钙测定)和51.3 Nm(β-Arrestin测定).评估相对于相关受体(包括p2X,P2Y和腺苷受体亚型以及外切核苷酸酶)的选择性.除了p2X1和p2X
DOI:10.1007/s11302-016-9542-3

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-7329515-B2
优先权日:2003-04-21
标题 :Solid support for the synthesis of 3′-amino oligonucleotides
发明人：LEUCK MICHAEL; WOLTER ANDREAS
权利人:SIGMA ALDRICH CO
摘要:The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules. The methods provided are particularly mild, do not require any modifications in standard protocols for the synthesis and deprotection of oligonucleotides, provide the 3′-amino oligonucleotides free of side products and do not introduce chiral centers to the oligonucleotides.

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.