专利号:US-2024101516-A1 优先权日:2021-01-20 标 题:Synthesis of polyfluorinated aryl and heteroaryl carboxamides 发明人:KADUSKAR RAHUL; BORATE KAILASKUMAR; ADHAV SUYOG; THIRUNAVUKKARASU SARAVANAN; SHINDE HARISH; GOETZ ROLAND 权利人:BASF SE 摘要:The presently claimed invention relates to a process for the preparation of mono-, di-, tri-, fluoro arylamide or hetroarylamide.
专利号:CN-102898360-A 优先权日:2012-11-12 标题 :Synthesis of 3,5-Dibromo-4-fluoropyridine
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:KR-20230134489-A 优先权日:2021-01-20 标题:Synthesis of polyfluorinated aryl and heteroaryl carboxamides
专利号:CN-116724021-A 优先权日:2021-01-20 标 题:Synthesis of polyfluorinated aryl and heteroaryl carboxamides
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.
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 15. 摘要:Sanz, R.; Su, Science of Synthesis: Knowledge Updates, (2024) 1, 133. 摘要:Wang, X.; Hu, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2. 摘要:Wang, X.; Hu, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.