CAS: 446-17-3; 2,4,5-Trifluorobenzoic Acid

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2,4,5-三氟苯腈置于硫酸体系中,化学反应 2.0H,反应生成 2,4,5-三氟苯甲酸
参考文献:喹诺酮类抗菌剂.8-取代的喹啉-3-羧酸和1,8-萘啶-3-羧酸的合成及构效关系.
标题:喹诺酮类抗菌剂.8-取代的喹啉-3-羧酸和1,8-萘啶-3-羧酸的合成及构效关系.
摘要:一系列7,8-二取代的1-环丙基-6-氟喹啉-3-羧酸,7-取代的1-环丙基-6-氟-1,8-萘啶-3-羧酸和10-取代的9-氟吡啶并苯并恶嗪已经制备了-6-羧酸并评估了其抗菌活性.在7-位(苯并恶嗪10-位)检测的侧链包括哌嗪基(g),3-氨基吡咯烷基(a),3-(氨基甲基)吡咯烷基(b)和烷基化的3-(氨基甲基)吡咯烷基(cf).喹诺酮环系统c-8的变异包括氢,硝基,氨基,氟和氯.8氢喹诺酮和1,8-萘啶上侧链对革兰氏阴性生物的体外活性的相对增强比cf更大,B更大,G更大.由8个取代基赋予取代的喹诺酮核的活性的顺序为:F大于cl大于萘啶大于h大于苯并恶嗪大于nh2大于no2.这些趋势在体内得以保留.
DOI:10.1021/jm00400A016

专利信息

专利号:US-6180830-B1
优先权日:1995-11-08
标题 :Method for preparing a bimetallic ruthenium/tin catalyst and a process for the synthesis of aldehydes
发明人：JACQUOT ROLAND
权利人:RHODIA CHIMIE SA
摘要:The present invention relates to a new process for the preparation of a bimetallic ruthenium/tin catalyst. The process for the preparation of a bimetallic ruthenium/tin catalyst according to the invention is characterised by the fact that it consists in carrying out the reduction of a ruthenium complex having an electrovalency of -4 and a coordination number of 6, the ligands being either a halogen atom or an anion or a tin halide. The catalyst is further employed for the preparation of aldehydes by reduction, in the vapor phase, of carboxylic acids, esters and anhydrides.

专利号:US-8765668-B2
优先权日:2010-06-04
标 题 :Methods of synthesis of β-aminobutyryl substituted compounds
发明人：STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO
权利人:STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO; LEK PHARMACEUTICALS
摘要:The present invention relates to process to prepare β-aminobutyryl compounds having β-amino acid core structural moieties and optionally having γ-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.

专利号:WO-9731891-A1
优先权日:1996-03-01
标 题:Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile
发明人：LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M
权利人:MERCK & CO INC; LYNCH JOSEPH E; SHI YAO JUN; WELLS KENNETH M
摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

专利号:EP-2397141-A1
优先权日:2010-06-16
标 题:Process for the synthesis of beta-amino acids and derivatives thereof
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to a process for the preparation of β-amino acids and derivatives thereof, which is especially suited for gliptins and particularly sitagliptin. A key step makes use of suitably derivatized epoxides or aziridines, which owing to a chirality provides a source of chirality for intermediates which are suitable for building up β-amino acids and similar compounds, in particular in the construction of the sitagliptin molecule.

专利号:US-11174266-B2
优先权日:2018-02-13
标 题 :Efficient process for the preparation of sitagliptin
发明人：SHI TERRY; LOU SAM; DE LUCCHI OTTORINO; PADOVAN PIERLUIGI
权利人:F I S —FABBRICA ITALIANA SINTETICI S P A
摘要:Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.

专利号:WO-2024126692-A1
优先权日:2022-12-15
标题 :Peracid promoters in the iridium-catalyzed hydrosilylation synthesis of haloalkylorganosilanes
发明人：SCHOLZ HENRIK; KROKE EDWIN; KRAUSHAAR KONSTANTIN; GLATZER HOLGER JÃœRGEN; LEWIS KENRICK MARTIN; WAGNER ROLAND
权利人:MOMENTIVE PERFORMANCE MAT GMBH
摘要:The present invention is directed at a process for producing a compound of Formula (I): (R1)y(R2O)3-ySiCH2CHR3CR4R5X comprising reacting (a) an olefinic halide; (b) an alkoxysilane; (c) a catalytically effective amount of iridium-containing catalyst; and (d) a reaction-promoting effective amount of a peroxycarboxylic acid to produce the product of Formula (I).