CAS: 348-51-6; 1-Chloro-2-Fluorobenzene

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2-氯苯甲酸置于tetrakis(Acetonitrile)Copper(I)Tetrafluoroborate,Tbaf(Tbuoh)4,Copper(II) Bis(Trifluoromethanesulfonate)体系中,用 乙腈 用作溶剂,化学反应 0.5H,以82%的收率获得2-氯氟苯
参考文献:苯甲酸的自由基脱羧碳金属化:芳族脱羧氟化的解决方案
标题:苯甲酸的自由基脱羧碳金属化:芳族脱羧氟化的解决方案
摘要:丰富的芳香羧酸存在于自然界和合成中的巨大结构多样性中.迄今为止,苯甲酸的具有合成价值的脱羧官能化主要是通过过渡金属催化的脱羧交叉偶联来实现的.然而,通常需要 140 oc 反应温度的热脱羧碳金属化的高活化能垒限制了底物范围以及可以维持这种条件的合适反应的范围.许多反应,例如,为脂肪族羧酸很好地开发的脱羧氟化,对于芳香族对应物来说,用当前的反应化学是无法实现的.这里,我们报告了一种概念上不同的方法,通过低势垒光诱导配体到金属电荷转移 (Lmct) 启用自由基脱羧碳金属化策略,该策略生成假定的高价芳基铜 (III) 配合物,从中可以发生通用的轻松还原消除.我们证明了我们的新方法适用于解决以前未实现的苯甲酸的一般脱羧氟化.
Doi:10.1021/jacs.1C02490

专利信息

专利号:US-2010016607-A1
优先权日:2006-12-11
标题:Process for the Synthesis of Highly Active Binary Metal Fluoride as a Fluorinating Agent for Aromatics
发明人：DOLBIER JR WILLIAM R; JANMANCHI KRISHNA MURTHY
权利人:UNIV FLORIDA
摘要:The subject invention relates to a process for the synthesis of highly active binary metal fluoride system for the fluorination of aromatic compounds. Fluorinated aromatic compounds are valuable synthons for the chemical synthesis of pharmaceutical drugs and novel polymers. Fluorobenzene is used to control carbon content in steel manufacturing, is an intermediate for pharmaceuticals, pesticides and other organic compounds. Fluorobenzene is typically produced by the reaction of aniline and sodium nitrite in the presence of hydrogen fluoride. The present invention relates to a process for the synthesis of highly active binary metal fluoride system consists of copper (II) fluoride and aluminum (III) fluoride for the fluorination of aromatic compounds in gas phase and recycling of the reagent, in situ, using O 2 and HF.

专利号:US-5512701-A
优先权日:1995-06-07
标题:Process for the synthesis of vinyl sulfenic acid derivatives
发明人：HOARD DAVID W; LUKE WAYNE D
权利人:LILLY CO ELI
摘要:The present invention is directed to a new process for the synthesis of vinyl sulfenic acid derivatives. These compounds are useful for the synthesis of benzo[b]thiophenes, in particular 2-aryl-benzo[b]thiophenes.

专利号:US-6995289-B2
优先权日:2000-08-02
标题 :Process for synthesis of alpha, beta-unsaturated ketones
发明人：PATEL IAN; HOPES PHILIP
权利人:ASTRAZENECA AB
摘要:A method for the synthesis of an α,β-unsaturated ketone useful for making substituted 1,4-dihydropyridines is described by reacting an aldehyde with pyrrolidine and then adding a ketone followed by trifluoroacetic acid at low temperature. The synthesis is used in a process for making substituted 1,4-dihydropyridines wherein a vinylogous amide is prepared by reacting a 1,3-cyclohexanedione with a phenylethylamine. The α,β-unsaturated ketone can be reacted with a vinylogous amide to form a 1,5-diketone which can be converted to a substituted 1,4-dihydropyridine.

专利号:US-10562872-B2
优先权日:2016-02-08
标 题 :Synthesis of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine
发明人：DINESS FREDERIK; MELDAL MORTEN; JACOBSEN CHRISTIAN BORCH
权利人:H LUNDBECK AS
摘要:The invention relates to a method for synthesis of 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]piperazine in the presence of a strong base.

专利号:US-9242965-B2
优先权日:2013-12-31
标题:Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
发明人：ZHENG JUNCHENG; DENG DA; LV GUANGHUA; YAN JUN; BRANDENBURG JOERG; KROEBER JUTTA; SCHOLZ ULRICH
权利人:BOEHRINGER INGELHEIM INT
摘要:The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I n nwherein R 1 and R 2 independently denote C 1-3 -alkyl groups and X − denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.

专利号:US-2023212204-A1
优先权日:2020-01-16
标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds
发明人：XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI
权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST
摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.