CAS: 371-40-4; 4-Fluoroaniline

上下游产品

1-Chloro-4-fluorobenzene 4-Fluorobenzoic acid N-Phenylhydroxylamine nitrobenzene (Z)-4-((4-fluorophenyl)amino)-4-oxobut-2-enoic acid N-(4-fluorophenyl)benzo[d]thiazol-2-amine 6-methyl-N-(4-fluorophenyl)benzo[d]thiazol-2-amine 2,5-bis-(4-fluoro-anilino)-[1,4]benzoquinone-bis-(4-fluoro-phenylimine)

📜4-氟苯硼酸置于sodium Hydroxide,Hydroxylamine-O-Sulfonic Acid体系中,用 乙腈 作为反应溶剂,化学反应 16.0H,以69%的收率获得产物4-氟苯胺
参考文献:从硼酸和普通+ Nh 2等同物到伯胺的无过渡金属通道.
标题:从硼酸和普通+ Nh 2等同物到伯胺的无过渡金属通道.
摘要:通过使用常见的廉价亲电氮源(h 2 N-Oso 3H,Hsa).通过这种方法发现富含电子的底物具有最高的反应性.但是,在室温条件下,即使是中等电子贫乏的基材也能很好地耐受.与不受阻碍的基材相比,受阻的基材似乎同样有效.高度缺乏电子的底物在室温下以非常低的产率提供产物,但是在回流温度下获得中等至非常好的产率.我们的方法也适用于几种常见的硼酸衍生物(例如频哪醇酯)的亲电胺化反应.我们证明了它可以与金属-卤素交换反应或各种定向的邻位金属化方案以"一锅"顺序结合使用,以合成具有独特取代模式的芳香胺.dft研究,结合实验结果,表明该反应通过碱介导的hsa活化发生的,然后发生1,2芳基b-n迁移.这种活化方式对于反应的成功似乎至关重要,并且首次允许在环境温度下对硼酸进行一般的亲电子胺化.
DOI:10.1021/jo5025078

专利信息

专利号:US-2013338369-A1
优先权日:2011-03-07
标 题 :Process for the Synthesis of Aminobiphenylene
发明人：HEINRICH MARKUS; PRATSCH GERALD
权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE
摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.

专利号:US-5932726-A
优先权日:1996-12-16
标 题 :Asymmetric synthesis of benzoxazinones
发明人：PIERCE MICHAEL ERNEST; CHOUDHURY ANUSUYA; PARSONS JR RODNEY LAWRENCE; RADESCA LILIAN ALICIA
权利人:DU PONT PHARM CO
摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

专利号:US-9902699-B2
优先权日:2012-10-24
标题 :Synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indenes
发明人：ROSOCHA GREGORY; BATEY ROBERT
权利人:ROSOCHA GREGORY; Gregory Rosocha
摘要:A procedure for the synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indene is described. The process involves the use of osmium tetroxide to cleave the indene double bond forming the keto aldehyde product, which is then combined with a substituted amine forming the substituted isoquinoline. Isoquinolines can be useful as industrial products in the chemical, agrochemical, oil and gas industry, as well as useful as medicaments in the pharmaceutical industry.

专利号:US-8383810-B2
优先权日:2004-12-20
标题:Process for the synthesis of azetidinones
发明人：THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L
权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L
摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

专利号:US-4973704-A
优先权日:1985-10-25
标题 :Pyrrolyl intermediates in the synthesis of pyrrole analogs of mevalonolactone and derivatives thereof
发明人：WAREING JAMES R
权利人:SANDOZ PHARMACEUTICALS CORP
摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R5, R6 and R7 are as defined below, R2 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R8, R9 and R10 are as defined below, R3 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R11, R12 and R13 are as defined below, R4 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R14, R15 and R16 are as defined below, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2-or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R17 is hydrogen or C1-3alkyl, and R18 is hydrogen, R19 or M, wherein R19 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, wherein each of R5, R8, R11 and R14 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy, each of R6, R9, R12 and R15 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each of R7, R10, R13 and R16 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy, with the provisos that (i) the -X-Z group is in the 2- or 3-position of the pyrrole ring, (ii) the -X-Z group is ortho to both R1 and R2 and (iii) R3 is ortho to R2, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.

专利号:US-9221821-B2
优先权日:2012-06-05
标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds
发明人：DIEP NHUT; KALYAN YURIY B
权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD
摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.