CAS: 1818-71-9; (2R,3R,4S,5R)-2-(6-Amino-2-Hydroxy-9H-Purin-9-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol

上下游产品

CAS号135041-24-6 6-[(4-甲基苯基)硫基]-... | CAS号2096-10-8 2-氨基腺苷 | CAS号16321-99-6 2',3',5'-三-O-乙酰... | CAS号35109-88-7 2-碘腺苷 | CAS号6974-32-9 1-乙酰氧基-2,3,5-三苯... | CAS号3373-53-3 异鸟嘌呤 | CAS号5987-76-8 2',3',5'-三-O-乙酰... | CAS号118-00-3 鸟苷 | CAS号6979-94-8 2',3',5'-三乙酰鸟苷

📜鸟苷置于甲醇,4-二甲氨基吡啶,二甲基十二/十四烷基叔胺,四乙基氯化铵,氨,Sodium Methylate,溶剂黄146,N,N-二甲基苯胺,Sodium Nitrite,三氯氧磷体系中,用 乙醇,水,乙腈 用作溶剂,化学反应 24.0H,反应生成巴豆苷
参考文献:2位取代的α,β-亚甲基adp衍生物:具有可变结合模式的强效竞争性ecto-5'-核苷酸酶(cd73)抑制剂.
标题:2位取代的α,β-亚甲基adp衍生物:具有可变结合模式的强效竞争性ecto-5'-核苷酸酶(cd73)抑制剂.
摘要:Cd73抑制剂是用于癌症(免疫)治疗的有前途的药物.在这里,我们介绍了合成,结构-活性关系,和竞争性cd73抑制剂α,β-亚甲基-Adp(aopcp)取代2位的新型衍生物的共晶体结构.小极性或亲脂性残基增加了效力,2-碘-和2-氯腺苷-5'-O-[(膦酰基甲基)膦酸](15,16)是对人cd73的ki值为3-的最有效抑制剂6 Nm.取决于2-取代基的大小和性质,通过x射线晶体学观测到可变的结合模式.取决于结合模式,发现了较大的物种差异,例如,2-哌嗪基-Aopcp(21)与人cd73相比,对大鼠cd73的效力低> 12倍.这项研究表明,只需将一个小的取代基引入aopcp的2位即可实现高cd73抑制力,而无需额外的大体积n6-取代基.此外,它为竞争性cd73抑制剂的结合模式提供了宝贵的见解,为药物开发提供了极好的基础.
Doi:10.1021/acs.Jmedchem.9B01611

专利信息

专利号:US-8138330-B2
优先权日:2006-09-11
标 题 :Process for the synthesis of oligonucleotides
发明人：LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED
权利人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED; SIGMA ALDRICH CO LLC
摘要:The present invention discloses novel methods for the synthesis of oligonucleotides with nucleoside phosphoramidites on solid supports. The methods comprise the stepwise chain assembly of oligonucleotides on supports with 5′-acyl phosphoramidites. The synthesis cycles consist of a front end deprotection step which is conducted with a solution of a primary amine or a phenolate, a phosphoramidite coupling step with a 5′-acyl nucleoside phosphoramidite in the presence of an activator, a phosphite oxidation step and an optional capping step. The novel methods improve the quality of synthetic oligonucleotides due to the irreversibility of the front end deprotection step, which prevents the formation of deletion sequences, and due to the avoidance of acidic reagents in the synthesis cycles, which prevent the formation of depurination side products. The invention further discloses novel nucleoside phosphoramidite compositions wherein the phosphoramidites carry acyl front end protective groups which are cleavable with primary amines or phenolates. The invention is applicable to the synthesis of oligodeoxyribonucleotides, oligoribonucleotides and oligonucleotides with modifications in their sugar or phosphate groups.

专利号:US-2009131651-A1
优先权日:2003-12-05
标题 :Synthesis of 2-substituted adenosines
发明人：BROWN GILES ALBERT; SAVORY EDWARD DANIEL; OUZMAN JACQUELINE VALERIE ANNE; STODDART ALISON MARGARET
权利人:BROWN GILES ALBERT; SAVORY EDWARD DANIEL; OUZMAN JACQUELINE VALERIE ANNE; STODDART ALISON MARGARET
摘要:Synthesis of 2-substituted adenosines of formula (I) using 2-nitro pentabenzoyl adenosine, or 2-nitro pentaacetyl adenosine, as intermediate is described: Formula (I) wherein R=C 1-6 alkoxy (straight or branched), a phenoxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF 3 —, cyano, nitro, C 1-4 alkyl, or C 1-4 alkoxy), a benzyloxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF 3 —, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy), or a benzoyl group (unsubstituted, or mono-, or di-substituted by halo, amino, CF 3 —, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy). The methods provide improved yield and purity of product.

专利号:US-7625735-B2
优先权日:1998-10-12
标 题:Recombinant kinase from insect cells for the synthesis of nucleoside monophosphates
发明人：IHLENFELDT HANS-GEORG; MUNCH-PETERSEN BRIGITTE; PISKUR JURE; SONDERGAARD LEIF
权利人:ROCHE DIAGNOSTIC OPERATIONS IN
摘要:A recombinant Drosophila melanogaster deoxynucleoside kinase that remains stable during the synthesis of nucleoside monophosphate without the addition of stabilizing SH reagents or stabilizing proteins, and that accepts all four natural deoxynucleotides is provided. In addition, the invention concerns DNA sequences, vectors, transformed cells, a method for production of the recombinant kinase as well as its use for preparing nucleoside monophosphates.

专利号:US-2019323050-A1
优先权日:2016-12-21
标题 :Modulation of Enzymatic Polynucleotide Synthesis Using Chelated Divalent Cations
发明人：GRISWOLD JR KETTNER JOHN FREDERICK; LEE HOWON; CHURCH GEORGE M
权利人:HARVARD COLLEGE
摘要:Methods and apparatus of modulating polynucleotide synthesis are provided. The methods include delivering reagents comprising enzymes, nucleotides and ions to oligonucleotide primers wherein the reagents catalyze incorporation of the nucleotides to 3′ ends of the oligonucleotide primers, and modulating incorporation of the nucleotides to the 3′ ends of the oligonucleotide primers. Polynucleotide synthesis is modulated by modulating presence or absence of catalytic cation cofactors to provide sequence defined synthesis of polynucleotides. In certain embodiments, the polynucleotides encode information.

专利号:US-8825411-B2
优先权日:2004-05-04
标 题:Design, synthesis and assembly of synthetic nucleic acids
发明人：GOVINDARAJAN SRIDHAR; MINSHULL JEREMY S; NESS JON E
权利人:GOVINDARAJAN SRIDHAR; MINSHULL JEREMY S; NESS JON E; DNA TWOPOINTO INC
摘要:Methods of synthesizing oligonucleotides with high coupling efficiency (>99.5%) are provided. Methods for purification of synthetic oligonucleotides are also provided. Instrumentation configurations for oligonucleotide synthesis are also provided. Methods of designing and synthesizing polynucleotides are also provided. Polynucleotide design is optimized for subsequent assembly from shorter oligonucleotides. Modifications of phosphoramidite chemistry to improve the subsequent assembly of polynucleotides are provided. The design process also incorporates codon biases into polynucleotides that favor expression in defined hosts. Design and assembly methods are also provided for the efficient synthesis of sets of polynucleotide variants. Software to automate the design and assembly process is also provided.

专利号:EP-0799313-A2
优先权日:1994-12-13
标 题 :Method and reagent for treatment of arthritic conditions, induction of graft tolerance and reversal of immune responses
发明人：BEIGELMAN LEONID; STINCHCOMB DANIEL T; JARVIS THALE; DRAPER KENNETH; PAVCO PAMELA; MCSWIGGEN JAMES; GUSTOFSON JOHN; USMAN NASSIM; WINCOTT FRANCINE; MATULIC-ADAMIC JASENKA; KARPEISKY ALEXANDER; THOMPSON JAMES D; MODAK ANIL; BURGIN ALEX
权利人:RIBOZYME PHARM INC
摘要:An enzymatic nucleic acid molecule which cleaves RNA associated with development or maintenance of an arthritic condition, induction of graft tolerance or reversal of an immune response. In particular, the ribozyme sequences are directed to an mRNA encoding B7-1, B7-2, B7-3, CD40 and/or stromelysin. Also provided are ribozymes where the uracil in positions 4 and/or 7 are substituted, as well as methods for the synthesis of 2'-alkylnucleotides, 2'-O-alkylthioalkyl, or 2'-alkylthioalkylnucleotides. The application further describes a method for diprotection of RNA with aqueous ethylamine, a method for synthesis of a basic ribonucleoside mimetics, and transcription units comprising an RNA polymerase II promoter, a U6 small nuclear promoter, or an adenovirus VA1 promoter system.