专利号:US-4699984-A 优先权日:1984-09-17 标 题 :Preparation of intermediates to 6-fluoro-7-(2,6-dimethylpyridyl)quinoline carboxylic acids and compounds 发明人:SINGH BALDEV 权利人:STERLING DRUG INC 摘要:Shown is the process which comprises heating 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid to produce a mixture of 4-(2-fluorophenyl)-2,6-dimethylpyridine and 2,4-dimethyl-5H-[1]benzopyrano[3,4-c]pyridin-5-one, separating the components of said mixture and nitrating 4-(2-fluorophenyl)-2,6-dimethylpyridine to produce 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Also shown are the 3-step synthesis of 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid from 2-fluorobenzaldehyde and the five step synthesis of 1-ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarboxylic acid, a highly potent antibacterial agent, starting with 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Other intermediates shown in said five step synthesis include 3-(2,6-dimethyl-4-pyridinyl)-4-fluorobenzeneamine and diethyl 4-fluoro-3-(2,6-dimethyl-4-pyridinyl)anilinomethylenemalonate.
专利号:US-2025170267-A1 优先权日:2022-02-28 标 题 :Antibody-drug conjugate precursor and intermediate for synthesis thereof 发明人:TSUZAKI YASUNORI; MIZUNO GEN; KASHIWAGI TAKAMASA; TANAKA MASAYUKI; SHIMIZU HAYATO; NONOUCHI SHIMPEI; MATSUSHITA TAKASHI; KIMURA TOMIO 权利人:UBE CORP 摘要:A method for improving the stability of an antibody-drug conjugate in a living body, and a conjugate precursor for producing a stabilized antibody-drug conjugate. An antibody-drug conjugate precursor represented by the following general formula (I) or a salt thereof, a synthetic intermediate thereof or a salt thereof, n Z-L-D  (I)n n where Z is a reactive group which can react with a functional group present in an antibody or a modified antibody; D is an antitumor drug residue in which one hydrogen atom or one hydroxy group is removed from any position of an antitumor drug molecule or an analog thereof or a derivative thereof; L is a linker which links Z to D; and at least any one of D and L has one or more lactonyl group(s) at any position(s) as substituent(s) or protecting group(s).
专利号:RU-2105007-C1 优先权日:1991-10-10 标题:Method of synthesis of benzo-[b]-naphthyridine derivatives and derivatives of benzo-[b]-naphthyridines
专利号:US-5442070-A 优先权日:1991-10-10 标 题:Derivatives of fluoro-quinoline carboxylic-3-acid and preparation therefor 发明人:DAUBIE CHRISTOPHE; LEGRAND JEAN-JACQUES; PEMBERTON CLIVE 权利人:BELLON LABOR SA ROGER 摘要:This invention relates to new derivatives of fluoro quinoline carboxylic-3 acid having general formula (I), ##STR1## wherein R is a hydrogen atom or an alkyl radical and Hal is a halogen atom, as well as salts thereof, when they exist, preparation thereof and utilization as synthesis intermediary.
专利号:US-10227344-B2 优先权日:2016-06-24 标题 :CK2 inhibitors, compositions and methods thereof 发明人:WEBBER STEPHEN E; TAO XUELIANG; BRIN ELENA 权利人:POLARIS PHARMACEUTICALS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. n nFor Formula (I) compounds R 1 , R 2 , R 3 , Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
专利号:CN-116396171-B 优先权日:2023-03-29 标题:A kind of synthesis method of 2-fluoro-5-nitrobenzaldehyde
[参考文献]: J Craig Ruble, Et Al. Synthesis Of (-)-Pnu-286607 By Asymmetric Cyclization Of Alkylidene Barbiturates. J Am Chem Soc. 2009 Mar 25;131(11):3991-7.
合成参考文献
摘要:Prager, R. H.; Williams, C. M., Science of Synthesis, (2005) 15, 1005. 摘要:Kikelj, D., Science of Synthesis, (2004) 16, 583.