CAS: 6974-78-3; 8-Bromo-7H-Purin-6-Amine

该化合物是一个合成核素模拟物,作为合成各种生物活性化合物的关键中间体,它具有很高的纯度和稳定性,使它在核酸研究和药物发现方面的研究应用具有理想性.该化合物为受体提供了特殊的特殊性,促进了分子生物学方面的定向研究.它在不同纯度和大小的可用性确保了各种实验装置的多功能性.

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CAS号66224-66-6 6H-Purin-6-imin... | CAS号6000-44-8 甘氨酸钠 | CAS号2946-39-6 8-溴腺苷 | CAS号14985-44-5 8-溴-2'-脱氧腺苷 | CAS号202136-43-4 8-溴-9-丁基-9h-嘌呤-6-胺 | CAS号2508-06-7 8-methylsulfany... | CAS号28128-33-8 8-氨基腺嘌呤 | CAS号30466-96-7 9H-Purin-6-amin... | CAS号17659-57-3 8-(3-nitropheny... | CAS号21149-26-8 8-羟基腺嘌呤 | CAS号696574-58-0 8-(3-methoxyphe... | CAS号827302-37-4 8-(3,4,5-trimet... | CAS号79270-98-7 8-azidoadenine

合成工艺路线路线简述

    📜8-溴-2'-脱氧腺苷置于水体系中,化学反应生成 8-溴腺嘌呤
    参考文献:Hydrolysis Of 2'-Deoxypurine Nucleosides. The Effect Of Substitution At The C-8 Position
    标题:Hydrolysis Of 2'-Deoxypurine Nucleosides. The Effect Of Substitution At The C-8 Position
    摘要:The Hydrolytic Stability Of 2'-Deoxypurine Nucleosides Is Decreased By Introduction Of Electron-Withdrawing Substituents At The C-8 Position In The Series Of Compounds 2-8,10-14. The Sulfone Group Causes A 2.9 X 10(4) Rate Acceleration For Glycosidic Bond Cleavage In Compound 14.
    DOI:10.1016/s0040-4039(00)73300-4

    专利信息


    专利号:US-9920084-B2
    优先权日:2011-08-23
    标题 :Ionic tags for synthesis of oligoribonucleotides
    发明人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK-HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER
    权利人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER; THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIV; HONG KONG POLYTECHNIC UNIV
    摘要:The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

    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: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.

    专利号:US-5877278-A
    优先权日:1992-09-24
    标题:Synthesis of N-substituted oligomers
    发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
    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 solid support-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. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

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    合成参考文献


    参考文献:10.1007/s003440010042
    摘要:Armstrong DJ. Folke K. Skoog: In Memory and Tribute. J Plant Growth Regul. 2002 Mar;21(1):3–16. doi: 10.1007/s003440010042.
    参考文献:10.1016/j.bmcl.2006.06.017
    摘要:Jin G, Wu CCN, Tawatao RI, Chan M, Carson DA, Cottam HB. Synthesis and immunostimulatory activity of 8-substituted amino 9-benzyladenines as potent Toll-like receptor 7 agonists. Bioorganic & Medicinal Chemistry Letters. 2006 Sep;16(17):4559–63. doi: 10.1016/j.bmcl.2006.06.017.
    参考文献:10.1016/0006-2952(95)02070-5
    摘要:Naguib FN, Iltzsch MH, el Kouni MM, Panzica RP, el Kouni MH. Structure-activity relationships for the binding of ligands to xanthine or guanine phosphoribosyl-transferase from Toxoplasma gondii. Biochem Pharmacol. 1995 Nov 09;50(10):1685–93. doi: 10.1016/0006-2952(95)02070-5.
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