CAS: 401815-98-3; (2-Fluoropyridin-4-yl)Boronic Acid

相似化合物

458532-86-0 401816-16-8 1263375-23-0

上下游产品

CAS号5419-55-6 硼酸三异丙酯 | CAS号128071-98-7 4-溴-2-氟吡啶 | CAS号22282-70-8 2-氟-4-碘吡啶 | CAS号688-74-4 硼酸三丁酯 | CAS号361147-25-3 2-氯-4-(2-氟吡啶-4-基)嘧啶

4-溴-2-氟吡啶置于正丁基锂,四甲基乙二胺,硼酸三异丙酯,Sodium Hydroxide体系中,用 乙醚,水 作为反应溶剂,化学反应 0.5H,以64%的收率获得产物2-氟-4-吡啶硼酸
参考文献:新型卤代吡啶基硼酸和酯的合成.第3部分:2或3-卤代吡啶-4-基硼酸和酯
标题:新型卤代吡啶基硼酸和酯的合成.第3部分:2或3-卤代吡啶-4-基硼酸和酯
摘要:本文描述了用于合成和一般的方法的新的2-,或3-卤代吡啶-4-基硼酸和酯隔离12-14,18-20.考虑到使用n Buli进行区域选择性的卤素金属交换或使用lda进行定向原金属化并随后从适当的单或二卤代吡啶开始用三异丙基硼酸酯淬灭,制备这些化合物.迄今为止研究的所有底物均提供单一的区域异构硼酸或酯产物.另外,已经发现这些化合物与一系列的芳基卤化物进行了pd催化的偶联,并授权了一种制备新吡啶库的策略.
DOI:10.1016/s0040-4020(02)00416-7

专利信息

专利号:WO-2023086799-A1
优先权日:2021-11-09
标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists
发明人：HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula 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.

专利号:US-8178559-B2
优先权日:2004-12-30
标 题:Organic compounds
发明人：BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI
权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.