CAS: 401816-16-8; (2,6-Difluoropyridin-4-yl)Boronic Acid

相似化合物

1204333-58-3 401815-98-3 1263375-23-0

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CAS号903513-58-6 4-溴-2,6-二氟吡啶 | CAS号5419-55-6 硼酸三异丙酯 | CAS号685517-71-9 2,6-二氟-4-碘吡啶 | CAS号121-43-7 硼酸三甲酯 | CAS号108-18-9 二异丙胺

2,6-二氟-4-溴吡啶,硼酸三异丙酯置于正丁基锂体系中,用 四氢呋喃,正己烷,甲苯 作为反应溶剂,以33%的收率获得产物2,6-二氟吡啶-4-硼酸
参考文献:Substituted Pyridines
标题:Substituted Pyridines
摘要:提供了一类包括新颖化合物的2,4-;2,3,4-;2,4,6-;2,3,4,5,6-取代吡啶.这些取代是通过本文披露的方法实现的,其中金属化的吡啶与亲电试剂发生反应.适当的亲电试剂包括co2,So2,二烷基碳酸酯,脲,甲酰胺,酰胺,羧酸酯,单烷基和二卤代烷基,氯,氟,溴和碘等卤素,金属盐,磺酮,磺酰基,醛,酮,酸酐,亚硝酸盐和亲电硼化合物,包括但不限于硼三烷氧化物和硼三卤化物.该发明更具体地披露了一种合成2,6-二氟吡啶-4-基硼酸的方法,包括:(1)将2,4,6-三氟吡啶与单水合肼反应,反应生成2,6-二氟-4-肼基吡啶,(2)将2,6-二氟-4-肼基吡啶与元素溴反应,反应生成4-溴-2,6-二氟吡啶,(3)将4-溴-2,6-二氟吡啶与有机锂化合物和硼酸盐在约0oc以下的温度下反应,反应生成2,6-二氟吡啶-4-基硼酸,其中所述过程在有机溶剂中进行.

专利信息

专利号:US-2009306392-A1
优先权日:2007-10-19
标题 :Gsm intermediates
发明人：HO CHIH YUNG
权利人:HO CHIH YUNG
摘要:The present invention relates the use of compounds having the general Formula I, wherein the definitions or R 1 and R 2 are provided in the specification. Said compounds of Formula I are useful for the synthesis of a variety of γ-secretase modulators, which are in turn useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.

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.