CAS: 903513-62-2; (2-Aminopyridin-4-yl)Boronic Acid

该化合物是一种多用途的boronic酸衍生物,广泛用于铃木-宫浦交叉反应,这是有机合成中构建碳-碳联系的关键方法.氨基氨基化合物和环上的碳酸酸碱都存在,这增强了其在催化变异变中的回作用性和选择性.该化合物在制药和农用化学研究中特别有用,因为它是七环化合物的建筑块.在温和条件下,与各种功能组相兼容,其稳定性使其成为复杂的分子合成的可靠试剂.建议在惰性条件下进行适当处理以保持其再活动性.

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相似化合物

1195995-72-2 903513-59-7 1207749-70-9

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CAS号19798-80-2 2-氨基-4-氯吡啶

合成工艺路线路线简述

  • 19798-80-2 = 903513-62-2
    反应条件:1.1 Reagents: Potassium Acetate,Bis(Pinacolato)Diborane Catalysts: Bis(Dibenzylideneacetone)Palladium,X-Phos Solvents: 1,4-Dioxane; 110 °C
    标题:Syntheses Of Novel 2,3-Diaryl-Substituted 5-Cyano-4-Azaindoles Exhibiting C-Met Inhibition Activity
    作者:Koolman,Hannes; Heinrich,Timo; Boettcher,Henning; Rautenberg,Wilfried; Reggelin,Michael
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2009 卷标:19(7) 页码:1879-1882
📜2-氨基-4-氯吡啶置于2-双环己基膦-2',6'-二甲氧基联苯,Tris-(Dibenzylideneacetone)Dipalladium(0),Potassium Acetate,联硼酸频那醇酯体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 3.0H,以100%的收率获得产物2-氨基吡啶-4-硼酸
参考文献: 6,7-Dihydropyrazolo[1,5-A]Pyrazin-4(5H)-One Compounds And Their Use As Negative Allosteric Modulators Of Mglur2 Receptors[fr] Composés 6,7-Dihydropyrazolo[1,5-A]Pyrazin-4(5H)-One Et Leur Utilisation Comme Modulateurs Allostériques Négatifs Des Récepteurs Mglur2
标题: 6,7-Dihydropyrazolo[1,5-A]Pyrazin-4(5H)-One Compounds And Their Use As Negative Allosteric Modulators Of Mglur2 Receptors[fr] Composés 6,7-Dihydropyrazolo[1,5-A]Pyrazin-4(5H)-One Et Leur Utilisation Comme Modulateurs Allostériques Négatifs Des Récepteurs Mglur2
摘要:本发明涉及一种新型的formula (I)的6,7-二氢吡唑并[1,5-A]吡嗪-4(5H)-酮衍生物,作为代谢型谷氨酸受体亚型2 ("Mglur2")的负变构调节剂(nams).该发明还涉及包含这些化合物的药物组合物,用于制备这些化合物和组合物的方法,以及用于预防或治疗涉及代谢型受体亚型2的疾病的化合物和组合物的用途,特别是中枢神经系统疾病.

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专利信息


专利号:US-7485725-B1
优先权日:2004-11-12
标 题:Substituted pyridines
发明人:CEFALO DUSTIN R; HENDERSON JASON I; MOKRI HOMAYOUN H
权利人:FRONTIER SCIENT INC
摘要:A class of 2,4-; 2,3,4-; 2,4,6-; 2,3,4,5,6-substituted pyridines is provided which include novel compounds. The substitutions are achieved according to methods disclosed herein in which a metallated pyridine is reacted with an electrophile. Suitable electrophiles include CO 2 , SO 2 , dialkylcarbonates, ureas, formamides, amides, carboxylic acid esters, mono- and dihaloalkyls, halogens such as chlorine, fluorine, bromine, and iodine, metallic salts, sulfones, sulfonyls, aldehydes, ketones, anhydrides, nitriles, and electrophilic boron compounds including, but not limited to, boron trialkoxides and boron trihalides. The subject invention more specifically discloses a process for the synthesis of 2,6-difluoropyridin-4-ylboronic acid which comprises: (1) reacting 2,4,6-trifluoropyridine with hydrazine monohydrate to produce 2,6-difluoro-4-hydrazinopyridine, (2) reacting the 2,6-difluoro-4-hydrazinopyridine with elemental bromine to produce 4-bromo-2,6-difluoropyridine, and (3) reacting the 4-bromo-2,6-difluoropyridine with an organolithium compound and a borate at a temperature of less than 0° C. to produce the 2,6-difluoropyridin-4-ylboronic acid, wherein said process is conducted in an organic solvent.

专利号:US-7087755-B1
优先权日:2004-11-12
标 题 :Substituted pyridines
发明人:CEFALO DUSTIN R; HENDERSON JASON I; MOKRI HOMAYOUN H
权利人:FRONTIER SCIENT INC
摘要:A class of 2,4-; 2,3,4-; 2,4,6-; 2,3,4,5,6-substituted pyridines is provided which include novel compounds. The substitutions are achieved according to methods disclosed herein in which a metallated pyridine is reacted with an electrophile. Suitable electrophiles include CO 2 , SO 2 , dialkylcarbonates, ureas, formamides, amides, carboxylic acid esters, mono- and dihaloalkyls, halogens such as chlorine, fluorine, bromine, and iodine, metallic salts, sulfones, sulfonyls, aldehydes, ketones, anhydrides, nitrites, and electrophilic boron compounds including, but not limited to, boron trialkoxides and boron trihalides. The subject invention more specifically discloses a process for the synthesis of 2,6-difluoropyridin-4-ylboronic acid which comprises: (1) reacting 2,4,6-trifluoropyridine with hydrazine monohydrate to produce 2,6-difluoro-4-hydrazinopyridine, (2) reacting the 2,6-difluoro-4-hydrazinopyridine with elemental bromine to produce 4-bromo-2,6-difluoropyridine, and (3) reacting the 4-bromo-2,6-difluoropyridine with an organolithium compound and a borate at a temperature of less than about 0° C. to produce the 2,6-difluoropyridin-4-ylboronic acid, wherein said process is conducted in an organic solvent.

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