CAS: 2240-25-7; 4-Amino-5-Bromopyrimidin-2(1H)-One

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5-bromo-2-methoxypyrimidin-4-amine Cytosine cytosine 6-amino-2-hydroxypyrimidine 1-(3,5-di-O-benzoyl-2-deoxy-2,2-difluoro-β-L-erythro-pentofuranos-1-yl)-5-brom°Cytosine 1-(3,5-di-O-benzoyl-2-deoxy-2,2-difluoro-α-L-erythro-pentofuranos-1-yl)-5-brom°Cytosine N-1-(p-toluenesulfonyl)cytosine Cytosine

📜胞嘧啶置于n-溴代丁二酰亚胺(Nbs),溶剂黄146体系中,化学反应 4.0H,以65.5%的收率获得5-溴胞嘧啶
参考文献:基于胞嘧啶的tet酶抑制剂.
标题:基于胞嘧啶的tet酶抑制剂.
摘要:Dna甲基化因其在调节局部基因转录中的关键作用而被称为prima Donna后生标记.整个基因组中dna甲基化景观的变化发生在细胞转变过程中,例如分化和神经元可塑性改变,并在疾病状态(例如癌症)中失调.已知tet酶家族负责催化反向过程,该过程是通过识别5-甲基胞嘧啶并通过fe(II)/α-酮戊二酸依赖性机制氧化甲基来进行的dna去甲基化.在这里,我们描述了新型基于胞嘧啶的tet酶抑制剂的设计,合成和评估,这是一类先前尚未开发但在表观遗传学领域中广泛需要的小分子探针.我们确定了一种有前途的基于胞嘧啶的先导化合物bobcat339,对tet1和tet2具有中等μm的抑制活性,但不抑制dna甲基转移酶dnmt3A.Tet酶活性位点的计算机模拟用于合理化bobcat339和其他基于胞嘧啶的抑制剂的活性.这些新的分子工具将对表观遗传学领域有用,并成为针对dna甲基化和基因转录的新疗法的起点.
Doi:10.1021/acsmedchemlett.8B00474

专利信息

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-10253153-B2
优先权日:2015-04-24
标题 :Linker and support for solid phase synthesis of nucleic acid, and production method of nucleic acid using said support
发明人：MAETA ERI; MORI KENJIRO; HORIE SHOHEI; ITO TAKAHIKO; SAITO SHOICHIRO; NAGAO RYUHEI
权利人:NITTO DENKO CORP
摘要:The present invention provides a linker for solid phase synthesis of nucleic acid, which consists of a compound represented by the formula (I) or the formula (II), a support for solid phase synthesis of nucleic acid, which has a structure represented by the formula (III), and a production method of a nucleic acid, which uses the support: n nwherein each symbol is as defined in the SPECIFICATION.

专利号:US-6022963-A
优先权日:1995-12-15
标 题:Synthesis of oligonucleotide arrays using photocleavable protecting groups
发明人：MCGALL GLENN H; NAM NGO QUOC
权利人:AFFYMETRIX INC
摘要:Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar-C(R1)(R2)-O-C(O)- wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar-C(R1)(R2)-O-C(O)- via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1=R2=H, X is not linked to Ar-C(R1)(R2)-O-C(O)- via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the 'PYMOC' protecting group, pyrenylmethyloxycarbonyl, where Ar=pyrenyl and R1=R2=H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.

专利号:WO-2023039068-A1
优先权日:2021-09-08
标题:Compositions and methods for synthesis of peptide nucleic acid intermediates
发明人：COULL JAMES M; GILDEA BRIAN D
权利人:NEUBASE THERAPEUTICS INC
摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.

专利号:WO-2024185775-A1
优先权日:2023-03-06
标 题:Long-chain alkenyloxy–substituted benzoyl derivative and oligonucleotide synthesis method using same
发明人：OKADA YOHEI; INANAGA KAZATO; SHOJI Yukiya; MIZUFUNE HIDEYA; SUDO TATSUYA; ADACHI Sota; HOSOI Kazushi
权利人:SPERA PHARMA INC; TOKYO UNIV OF AGRICULTURE AND TECHNOLOGY
摘要:The purpose of the present invention is to provide a novel pseudo–solid phase protecting group that can be used in liquid-phase oligonucleotide synthesis. The purpose of the present invention is also to provide an oligonucleotide synthesis method that uses a novel pseudo–solid phase protecting group.　The present invention provides a compound represented by formula (1) (in which R represents a C14–60 alkenyl group, n represents 2 or 3, m represents 0 or 1, p represents 1 or 2, X represents C, N, O, or S, Y represents a single bond or B(CH 2 ) t * or may form a ring with X, and Z represents a single bond or (CH 2 ) s (s being an integer from 1 to 5)). The present invention also provides an oligonucleotide production method that uses the compound.

专利号:WO-2024163733-A1
优先权日:2023-02-01
标题:Electrochemical synthesis with redox stable nucleotides
发明人：WU TIANDI; LACKEY JEREMY; LIN YANYOU; PITSCH STEFAN
权利人:TWIST BIOSCIENCE CORP
摘要:Provided herein are compositions, devices, systems and methods for constructing and storing polynucleotides encoding information with redox resistant bases. The compositions, devices, systems, and methods described herein provide for storage or synthesis of a library comprising a plurality of polynucleotides with one or more redox resistance bases. Further provided herein are methods to increase DNA synthesis yield and fidelity.