CAS: 461-96-1; 1-Bromo-3,5-Difluorobenzene

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CAS号6303-21-5 次磷酸 | CAS号101471-20-9 2-溴-4,6-二氟苯胺氢溴酸 | CAS号1435-51-4 1,3-二溴-5-氟苯 | CAS号444-14-4 2-溴-4,6-二氟苯胺 | CAS号1317-39-1 氧化亚铜 | CAS号367-25-9 2,4-二氟苯胺 | CAS号372-18-9 1,3-二氟苯 | CAS号651027-02-0 (2,6-difluoroph... | CAS号651027-03-1 (3-bromo-2,6-di... | CAS号372-18-9 1,3-二氟苯 | CAS号108-90-7 氯苯 | CAS号100-47-0 苯甲腈 | CAS号455-40-3 3,5-二氟苯甲酸 | CAS号32085-88-4 3,5-二氟苯甲醛 | CAS号445491-09-8 (3,5-二氟苯基乙炔基)三甲基硅烷 | CAS号433939-27-6 3-氟-5-溴苯酚 | CAS号207462-72-4 3-(3,5-DIFLUORO... | CAS号103-50-4 二苄醚 | CAS号84315-24-2 3-(3,5-二氟苯基)丙酸

1,3-二氟苯置于potassium Fluoride,正丁基锂,溴,仲丁基锂,二异丙胺体系中,用 四氢呋喃,乙醚,正己烷,环己烷,水 作为反应溶剂,化学反应 5.0H,反应生成 1-溴-3,5-二氟苯
参考文献:探索结构机遇:1,3-二氟苯的区域柔性取代
标题:探索结构机遇:1,3-二氟苯的区域柔性取代
摘要:为了证明现代有机金属方法的优越性,廉价的起始材料 1,3-二氟苯已被选择性地转化为三种苯甲酸和所有七种溴苯甲酸.同位上的两个氟原子.制备2,6-二氟苯甲酸.在由直接金属化和羧化组成的一锅反应中.3-溴-2,6-二氟苯甲酸路线的关键步骤是去质子化引发的溴从2-位迁移到4-位.所有其他产品均通过(2,6-二氟苯基)三乙基硅烷获得.与氟原子相邻的位点连续去质子化,然后进行适当的亲电取代,不仅提供 5-溴-2,4-二氟苯甲酸,还提供 3,5-二溴-2,6-二氟苯基三乙基硅烷及其 5-碘类似物.这些反过来产生 3,4-二溴-2,6-二氟苯基三乙基硅烷 (I) 和它的 4-碘类似物在最重的卤素的碱介导迁移后产生 2-溴-4,6-二氟苯甲酸和 2-溴-3,5-二氟苯甲酸可直接获得.中间体 I 的区域受控单脱溴提供了(4-溴-2,6-二氟)三乙基硅烷,这开辟了通过羧化和原脱甲硅烷化反应生成 3,5-二氟苯甲酸和
DOI:10.1002/ejoc.200300354

专利信息

专利号:US-2007238878-A1
优先权日:2004-10-13
标 题 :Process for the synthesis of 4-(3-sulfonylphenyl)-piperidines
发明人：DESMOND RICHARD; DEVINE PAUL N; SONESSON CLAS; GAUTHIER DONALD R
权利人:DESMOND RICHARD; DEVINE PAUL N; SONESSON CLAS; GAUTHIER DONALD R
摘要:The present invention is directed to processes for the preparation of 4-(sulfonylphenyl)-piperidines of the Formula (VI), and pharmaceutically acceptable salts thereof; which comprises oxidizing a sulfide of the Formula (VII) or Formula (VIII), to give a compound of the Formula (IX) or Formula (X) respectively, followed by catalic reduction of the compound of the Formula (IX) or dehydration of compound of formula (X) to give a compound of Formula (IX) followed by catalytic reduction of the compound formula (IX) to give the compound of the Formula (VI).

专利号:US-9365494-B2
优先权日:2008-12-18
标 题 :Process for synthesis of amino-methyl tetralin derivatives
发明人：DURKIN KIERAN; FISHER LAWRENCE EMERSON; MEILI ARTHUR; SCALONE MICHAELANGELO; SHI XIANQING; VITALE JUSTIN
权利人:DURKIN KIERAN; FISHER LAWRENCE EMERSON; MEILI ARTHUR; SCALONE MICHAELANGELO; SHI XIANQING; VITALE JUSTIN; ROCHE PALO ALTO LLC
摘要:Methods for producing a compound of formula k1 or k2 n nby reducing a dihydronapthalene amide compound of formula in n nwith hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2n nRu(Z) 2 (L)  j1;n nRu(E)(E′)(L)(D)  j2;n nwherein m, n, Ar, Y, R 1 E, E′, D, Z and L are as defined herein.

专利号:US-6825185-B2
优先权日:2000-12-21
标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D
权利人:NITROMED INC
摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-5789624-A
优先权日:1995-05-30
标题:Synthesis of and hydroformylation with fluoro-substituted bidentate phosphine ligands
发明人：UNRUH JERRY D; SEGMULLER BRIGITTE E; CHAPA GABRIEL R; PRYOR KENT E
权利人:HOECHST CELANESE CORP
摘要:Hydroformylation of alkenes to aldehydes in the presence of a rhodium complex catalyst is improved by the addition of a novel bidentate ligand of the formula ##STR1## wherein R 1 , R 2 , R 1 ' and R 2 ' are organic radicals selected from alicyclic, aliphatic and aromatic groups of which at least one is preferably substituted with at least one electronegative moiety and the methylene groups are present at the trans-2,3 positions on the norbomane moiety. The invention also provides a novel method for producing the bidentate ligand and novel intermediate phosphine oxide and phosphinous acid compounds.

专利号:US-6774125-B2
优先权日:1998-06-22
标 题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-6509331-B1
优先权日:1998-06-22
标题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.