CAS: 903513-58-6; 4-Bromo-2,6-Difluoropyridine

该化合物是一种环环状芳烃化合物,其特点是用溴和氟原子取代了环,这种环状环状芳烃化合物的存在对卤素替代物的化学特性,包括反应性和极度有重大影响,包括反应性和极度.这种化合物通常呈现黄色至浅褐色的灰色外观,在乙醇和丙酮等有机溶剂中溶解,但因其非极性特性,在水中溶解较少.溴原子引入了一个更大的原子半径,可以参与各种化学反应,例如核细胞替代物,而氟质替代物则会增强分子的电镀性质,影响其酸性和基本性.4-Bromo-2,6-二氟丙烯丁胺经常用于制药和农业化学研究,作为合成更复杂分子的建筑块块.其独特的卤素亚种化合物组合允许在医药化学中应用多种用途,特别是在研制化合物中,特别是用于核循环替代物,而氟质替代物则会增强分子的电镀特性.

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128071-98-7 1513-65-1 766-11-0

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CAS号401816-16-8 2,6-二氟吡啶-4-硼酸

合成工艺路线路线简述

  • 3512-17-2 = 903513-58-6
    反应条件:1.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Tetrahydrofuran; 2 H,50 °C1.2 Reagents: Bromine Solvents: Chloroform; 6 H,Reflux
    标题:Towards Libraries Of Luminescent Lanthanide Complexes And Labels From Generic Synthons
    作者:Starck,Matthieu; Kadjane,Pascal; Bois,Emmanuel; Darbouret,Bruno; Incamps,Anne; Et Al
    参考文献:Chemistry - A European Journal 日期:2011 卷标:17(33) 页码:9164-9179
📜2,6-二氟吡啶-4-硼酸频哪醇酯置于copper(Ll) Bromide体系中,用 甲醇,水 作为反应溶剂,化学反应 1.5H,反应生成 2,6-二氟-4-溴吡啶
参考文献: Process For Preparing 1-[(3R,4S)-4-Cyanotetrahydropyran-3-Yl]-3-[(2-Fluoro-6-Methoxy-4-Pyridyl)Amino]P Yrazole-4-Carboxamide[fr] Procédé De Préparation De 1-[(3R,4S)-4-Cyanotétrahydropyran-3-Yl]-3-[(2-Fluoro-6-Méthoxy-4-Pyridyl)Amino]Pyrazole-4-Carboxamide
标题: Process For Preparing 1-[(3R,4S)-4-Cyanotetrahydropyran-3-Yl]-3-[(2-Fluoro-6-Methoxy-4-Pyridyl)Amino]P Yrazole-4-Carboxamide[fr] Procédé De Préparation De 1-[(3R,4S)-4-Cyanotétrahydropyran-3-Yl]-3-[(2-Fluoro-6-Méthoxy-4-Pyridyl)Amino]Pyrazole-4-Carboxamide
摘要:该申请涉及制备1-[(3R,4S)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺(i)的过程,包括(i)溴和碘吡啶中间体的合成,(II)可以以对映纯形式获得的吡唑酯中间体的合成,以及(iii)将这些中间体组合成化合物(i).

海关参考信息

专利信息


专利号:WO-2020118597-A1
优先权日:2018-12-13
标 题 :Process for making 1- [ (3r, 4s) -4-cyanotetrahydropyran-3-yl] -3- [ (2-fluoro-6-methoxy-4-pyridyl) amino] pyrazole-4-carboxamide
发明人:CHASSAING CHRISTOPHE PIERRE ALAIN; YIN JINGJUN; CLEATOR EDWARD; SONG LICHEN; XIAO WENSONG; DAHMEN THOMAS; SALANTA DANIEL; SCHEIPERS CLAUDIA; SCHMITT HARALD
权利人:INTERVET INT BV; INTERVET INC; CHASSAING CHRISTOPHE PIERRE ALAIN; YIN JINGJUN; CLEATOR EDWARD; SONG LICHEN; XIAO WENSONG; DAHMEN THOMAS; SALANTA DANIEL; SCHEIPERS CLAUDIA; SCHMITT HARALD
摘要:New processes for the preparation of 1- [ (3R, 4S) -4-cyanotetrahydropyran-3-yl] -3- [ (2-fluoro-6-methoxy-4-pyridyl) amino] pyrazole-4-carboxamide (I) which include (i) novel more efficient synthesis for bromo and iodo pyridine intermediates, (ii) synthesis of a novel pyrazole ester intermediate which can be obtained in enantiopure form and (iii) the combination of these intermediates into compound (I).

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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合成参考文献


参考文献:10.1007/978-3-319-04435-4_1
摘要:Shestopalov AM, Rodinovskaya LA, Mortikov VY, Fedorov AE. Synthesis of Fluorinated Pyridines. 2014. In: Fluorine in Heterocyclic Chemistry Volume 2. : Springer International Publishing; 2014.
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