CAS: 5570-18-3; (2-Aminophenyl)Boronic Acid

该化合物是一种有机有机体化合物,其特点是存在一个与2-氨基苯基混合物相连的有机酸功能组,该化合物一般是白色至白色固态,可溶解于可形成氢联结的碳酸组,可溶于水和酒精等极溶剂中.该化合物具有boronic酸的典型特性,包括能够与二醇形成可逆共价结合,使其在有机合成,药用化学等各种应用中有用,并成为制药业发展的一个构件.芳香环上的氨基酸组可参与进一步的化学反应,增强其多功能性.此外,B-2-(2-氨基苯基)bororonoron酸可以作为离子体,在协调化学中经常用于复合复杂的有机分子的合成中,例如铃木-米亚拉交配等,从而在诸如有机合成,药合成等多种应用中有用,其再活性和功能化潜力在工业应用中成为宝贵的化合物.

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CAS号5570-19-4 2-硝基苯基硼酸 | CAS号98-80-6 苯硼酸 | CAS号191171-55-8 2-氨基苯硼酸频哪醇酯 | CAS号7697-37-2 硝酸 | CAS号111609-76-8 3-nitrophenanth... | CAS号90-41-5 2-氨基联苯 | CAS号553-03-7 3,4-二氢-2(1H)-喹啉酮 | CAS号229-87-8 菲啶 | CAS号86-74-8 咔唑 | CAS号95-55-6 邻氨基苯酚 | CAS号95-54-5 邻苯二胺(OPD) | CAS号612-96-4 2-苯基喹啉 | CAS号24224-30-4 3-甲基-9H-咔唑-2-醇 | CAS号26844-83-7 6(5H)-Phenanthr...

合成工艺路线路线简述

  • 合成目标产物 2-Aminophenylboronic Acid 主要起始原料 2-Iodoaniline And Water And Bis(Pinacolato)Diboron
  • (文献来源)合成步骤主要原料 2-Iodoaniline 和 Water 和 Bis(Pinacolato)Diboron
2-氨基苯硼酸频哪醇酯置于三氯化硼体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,以52%的收率获得产物2-氨基苯硼酸
参考文献:轴向手性抗有丝分裂联芳基的不对称合成,通过atropo-对映选择性suzuki交叉偶联.
标题:轴向手性抗有丝分裂联芳基的不对称合成,通过atropo-对映选择性suzuki交叉偶联.
摘要:描述了轴向手性桥联联芳基(-)-2(具有原始抗有丝分裂特性的天然(-)-Rhazinilam的结构类似物)的催化不对称合成.关键步骤是分子间不对称suzuki偶联,使用双萘配体7A为(-)-2的前体非桥接联芳基(-)-6提供高达40%ee.在该反应中,筛选了各种已知的或新的联萘基和二茂铁基膦以及膦烷作为配体,并对其条件进行了优化.与另一个suzuki偶联系统的比较表明7A是迄今为止描述的这种类型转化最通用的配体.这项工作将不对称suzuki偶联首次应用于生物学相关的靶标.
DOI:10.1021/jo034298Y

专利信息


专利号:US-2004038331-A1
优先权日:2002-08-23
标题:Solid phase synthesis of biomolecule conjugates
发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; BRILLHART KURT L
摘要:Processes for the solid state phase formation synthesis of biomolecule conjugates, particularly protein-oligonucleotide conjugates are shown. One of the protein or oligonucleotide is reversibly bound to a solid substrate phase. At least one portion of each of the protein and the oligonucleotide molecules is activated with complementary activation groups. The activated protein and the activated oligonucleotide are then reacted, in a buffered solution resulting in the formation of the desired conjugate which remains reversibly bound to the substrate. The nature of the buffered solution is then modified causing the conjugate to be released from the substrate solid phase.

专利号:US-6919382-B2
优先权日:2000-08-31
标 题 :Preparation and uses of conjugated solid supports for boronic acids
发明人:HALL DENNIS G
权利人:UNIV ALBERTA
摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.

专利号:US-2023212216-A1
优先权日:2019-12-20
标 题:Synthesis of lactone derivatives and their use in the modification of proteins
发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH
权利人:GENIE BIOTECH UK LTD
摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

专利号:EP-1314727-B1
优先权日:2001-11-23
标题 :Direct synthesis of quaternary phenanthridinium salts
发明人:CAPELLE NICOLAS; GALLO ROGER
权利人:MERIAL SAS
摘要:Process for the preparation of phenanthridinium quaternary salts (I) comprises reacting a halo-aromatic compound (II) with a phenyl boronic derivative (III) in a basic medium, in the presence of a palladium catalyst. Process for the preparation of phenanthridinium quaternary salts of formula (I) comprises reacting a halo-aromatic compound of formula (II) with a phenyl boronic derivative of formula (III) in a basic medium, in the presence of a palladium catalyst. R<3>, R<8> = an electro-attractor group having an electronegativity at last equal to that of nitro; R<5> = a non-chemically labile group; R<6> = aryl or 5-12C heteroaryl, which my be condensed and may have one or more hetero atoms; X<-> = a halide or hydrogen sulfate anion or a base joined to a mineral acid; X = halogen; R = H; R+R = a group of formula (i); n, n' = 0-4; R<9>, R<10> = H or 1-5C alkyl. Independent claims are also included for: (1) intermediates of formula (VI); and (2) the preparation of (VI). X1 = halogen.

专利号:WO-0112791-A1
优先权日:1999-08-12
标 题 :Dna shuffling of dioxygenase genes for production of industrial chemicals
发明人:SELIFONOV SERGEY A; NEWMAN LISA M
权利人:MAXYGEN INC; SELIFONOV SERGEY A; NEWMAN LISA M
摘要:This invention provides improved polypeptides, including dioxygenases, dehydrogenases, ligases and transferases that are useful for the biocatalytic synthesis of compounds such as α-hydroxycarboxylic acids, and aryl- and alkyl-hydroxy and carboxylic acid compounds. The polypeptides provided herein are improved in properties such as regioselectivity, enzymatic activity, stereospecificity, and the like. Methods for obtaining recombinant polynucleotides that encode these improved polypeptides are also provided, as are organisms that express the polypeptides and are thus useful for carrying out said biocatalytic syntheses. Also provided by the invention are methods for increasing said solvent resistance of organisms that are used in the synthetic methods.

专利号:US-6605430-B1
优先权日:1998-08-12
标题 :DNA shuffling of monooxygenase genes for production of industrial chemicals
发明人:AFFHOLTER JOSEPH A; DAVIS S CHRISTOPHER; SELIFONOV SERGEY A
权利人:MAXYGEN INC
摘要:This invention provides improved monoxygenases, dehydrogenases, and transferases that are useful for the biocatalytic synthesis of compounds such as α-hydroxycarboxylic acids, and aryl- and alkyl-hydroxy compounds. The polypeptides provided herein are improved in properties such as regioselectivity, enzymatic activity, stereospecificity, and the like. Methods for obtaining recombinant polynucleotides that encode these improved polypeptides are also provided, as are organisms that express the polypeptides and are thus useful for carrying out said biocatalytic syntheses. Also provided by the invention are methods for increasing said solvent resistance of organisms that are used in the synthetic methods.
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合成参考文献


摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 203.
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 116.
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 199.
摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22.
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