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2-Fluoroaniline 2,4,4,6-Tetrabromo-2,5-cyclohexadien-1-one 4-bromo-2-fluoronitrobenzene 4-bromo-aniline 2-(4-bromo-2-fluorophenylamin°Carbonyl)-1-cyclohexene-1-carboxylic acid (4-Bromo-2-fluoro-phenyl)-methoxymethyl-amine 4-bromo-6-fluorobenzonitrile 2-amino-5-bromo-3-fluorobenzenesulphonic acid合成工艺路线路线简述
- 合成目标产物 4-Bromo-2-Fluoroaniline 主要起始原料 2-Fluoroaniline
- (文献来源)合成步骤主要原料 2-Fluoroaniline
2-氟苯胺置于n-溴代丁二酰亚胺(Nbs)体系中,用 氯仿 作为反应溶剂,化学反应 2.0H,以90%的收率获得产物4-溴-2-氟苯胺
参考文献:Dyrk1A抑制剂的多种杂环双酚化合物的合成及体外评价
标题:Dyrk1A抑制剂的多种杂环双酚化合物的合成及体外评价
摘要:双特异性酪氨酸磷酸化相关激酶1A(dyrk1A)是一种双特异性蛋白激酶,可催化磷酸化和自身磷酸化.较高的dyrk1A表达与癌症有关,特别是与脑内存在的胶质母细胞瘤有关.我们在这里报告设计为新型dyrk1A抑制剂的新型杂环二酚衍生物的合成和生物学评估.根据dandy铅的结构修饰,制备了这些杂环,如苯并咪唑,咪唑,萘啶,吡唑-吡啶,联吡啶和三唑并吡嗪,并测试了它们抑制dyrk1A的能力.这些衍生物均未显示出明显的dyrk1A抑制作用,但提供了有关7-氮杂吲哚部分重要性的有价值的知识.
DOI:10.1016/j.Bmc.2018.10.034
专利信息
专利号:US-11040938-B2
优先权日:2016-07-27
标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts
发明人:MA BING; PAN SHUAI
权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH
摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:WO-2025215126-A1
优先权日:2024-04-12
标题:Synthesis of vidofludimus and its calcium salt
发明人:VITT DANIEL; IGLICAR PETRA; GEGE CHRISTIAN; Mühler Andreas; KOHLHOF HELLA; GRÖPPEL MANFRED
权利人:IMMUNIC AG
摘要:The invention relates to the process of preparation of 2-fluoro-4-(3-methoxyphenyl)aniline (3) as an intermediate. Said intermediate 2-fluoro-4-(3-methoxyphenyl)aniline (3) is obtained in a Suzuki coupling reaction from (3-methoxyphenyl)boronic acid (1) and 4-bromo-2-fluoro-aniline (2). The invention further relates to the synthesis of vidofludimus (5) from said intermediate 2-fluoro-4-(3-methoxy-phenyl)aniline (3) and from 1-cyclopentene-1,2-dicarboxylic anhydride (4). The invention further relates to the synthesis of vidofludimus calcium (6) from said vidofludimus (5) and from a calcium salt, preferably Ca(OH)2.
专利号:US-6235871-B1
优先权日:1997-12-03
标题:Synthesis of oligoarylamines, and uses and reagents related thereto
发明人:SINGER ROBERT A; SADIGHI JOSEPH P; BUCHWALD STEPHEN L; MACKEWITZ THOMAS
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The transition metal-catalyzed amination of aryl halides, in conjunction with an orthogonal protective group scheme, forms the basis of two routes to oligoaniline precursors. The oligoaniline precursors are soluble in a variety of common organic solvents, and are easily converted to the deprotected oligoanilines. The method allows the preparation of oligoanilines of even or odd chain lengths, and the incorporation of a variety of functional groups into the oligomers. Polyanilines of low polydispersity can also be prepared by this method.
专利号:US-9815816-B2
优先权日:2005-09-30
标 题 :Chemical process for the synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline
发明人:BLIXT JORGEN; GOLDEN MICHAEL DAVID; HOGAN PHILIP JOHN; MARTIN DAVID MICHAEL GLANVILLE; MONTGOMERY FRANCIS JOSEPH; PATEL ZAKARIYA; PITTAM JOHN DAVID; SEPENDA GEORGE JOSEPH; SQUIRE CHRISTOPHER JOHN; WRIGHT NICHOLAS CARTWRIGHT ALEXANDER
权利人:ASTRAZENECA AB; GENZYME CORP
摘要:The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilizing said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.
专利号:US-6465656-B2
优先权日:1999-10-21
标题 :Synthesis of 1,3,5-trisubstituted pyrazoles
发明人:ZHOU JIACHENG; OH LYNETTE MAY; CONFALONE PASQUALE N; LI HUI-YIN; MA PHILIP
权利人:BRISTOL MYERS SQUIBB PHARMA CO
摘要:A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described. n These compounds are useful as factor Xa inhibitors.
专利号:US-7365197-B2
优先权日:2000-12-29
标题 :Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines
发明人:BERGER DAN MAARTEN; BIRNBERG GARY HAROLD; WANG YANONG
权利人:WYETH CORP
摘要:This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.