CAS: 579476-63-4; (2-Methylpyridin-4-yl)Boronic Acid

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660867-80-1 846548-44-5 2819702-62-8

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CAS号660867-80-1 2-甲基吡啶-4-硼酸频哪酯 | CAS号22282-99-1 2-甲基-4-溴吡啶 | CAS号5419-55-6 硼酸三异丙酯

4-溴-2-甲基吡啶置于四羟基二硼,1,3-Bis[(Diphenylphosphino)Propane]Dichloronickel(II),N,N-二异丙基乙胺,三苯基膦体系中,用 乙醇 作为反应溶剂,化学反应 4.0H,反应生成 2-甲基-4-吡啶硼酸
参考文献:镍催化四羟基二硼 [b2(Oh)4] 卤化物和拟卤化物的硼化反应
标题:镍催化四羟基二硼 [b2(Oh)4] 卤化物和拟卤化物的硼化反应
摘要:芳基硼酸作为试剂和目标结构在各种有用的应用中变得越来越重要.最近,报道了使用原子经济的四羟基二硼(bba)试剂在钯催化下合成芳基硼酸.钯的高成本,加上钯和铜催化工艺的一些限制,促使我们开发一种替代方法.因此,已经制定了使用四羟基二硼(bba)对芳基和杂芳基卤化物和拟卤化物进行镍催化的硼基化反应.该反应被证明具有广泛的官能团耐受性并适用于许多杂环体系.据我们所知,这里提供的例子代表了在室温下进行的唯一有效的镍催化宫浦硼化反应.
DOI:10.1021/jo401104Y

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.