对氟甲苯置于四氯化碳,溴,铁粉体系中,化学反应生成 3-溴-4-氟甲苯 参考文献:Varma; Raman; Nilkantiah,Journal Of The Indian Chemical Society,1944,Vol. 21,P. 112,114 标题:Varma; Raman; Nilkantiah,Journal Of The Indian Chemical Society,1944,Vol. 21,P. 112,114
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-7205300-B2 优先权日:1997-12-31 标 题:Aryl fused azapolycyclic compounds 发明人:COE JOTHAM WADSWORTH; BROOKS PAIGE ROANNE PALMER 权利人:PFIZER 摘要:This invention is directed to compounds of the formula (I): n nand their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
专利号:US-4229368-A 优先权日:1978-05-04 标题 :Esters and thiolesters of unsaturated acids 发明人:ANDERSON RICHARD J; HENRICK CLIVE A 权利人:ZOECON CORP 摘要:Esters and thiolesters of α-substituted unsaturated acids, intermediates therefor, synthesis thereof, and the use of said esters and thiolesters and compositions thereof for the control of pests.
专利号:US-4225533-A 优先权日:1979-06-01 标题:Fluorobenzyl esters of cyclopropanecarboxylic acids 发明人:HENRICK CLIVE A 权利人:ZOECON CORP 摘要:Novel esters of ether and thioether substituted cyclopropanecarboxylic acids, synthesis thereof, and intermediates therefor, such esters being useful as pesticides.
专利号:US-4446075-A 优先权日:1980-02-22 标 题:Substituted bromofluorobenzene derivatives and process for its manufacture 发明人:EIGLMEIER KURT; KNIEPS REINHARD 权利人:RIEDEL DE HAEN AG 摘要:Substituted bromofluorobenzene, wherein the fluorine is in para-position and the bromine in meta-position to another substituent, is prepared by direct bromination of the corresponding fluorobenzene derivative. Bromination is advantageously carried out in the presence of a catalyst, preferably a metal or metal salt. The elementary bromine is used in an amount of 0.9 to 1.3 mols per mol of fluorobenzene derivative and the reaction temperature is between 20° and 200° C. The bromofluorobenzene derivatives are suitable for the synthesis of medicaments and plant protective agents.
专利号:US-7563900-B2 优先权日:2004-10-13 标 题:Process for the preparation N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methane sulfonamido-dibenzo[b,d]furan-1-carboxamide 发明人:GOPALAN BALASUBRAMANIAN; GHARAT LAXMIKANT A; CHANDRASEKHAR BATCHU; PILLAI BIJUKUMAR G 权利人:GLENMARK PHARMACEUTICALS SA 摘要:The present invention relates to a method of preparing N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof, such as its sodium salt, and novel intermediate compounds useful in the synthesis of the aforementioned compound.
[参考文献]: G Vaidyanathan, Et Al. No-Carrier-Added (4-Fluoro-3-[131I]Iodobenzyl)Guanidine And (3-[211At]Astato-4-Fluorobenzyl)Guanidine. Bioconjug Chem. 1996 Jan-Feb;7(1):102-7.
合成参考文献
摘要:Dong, X.; Liu , H., Science of Synthesis Knowledge Updates, (2019) 3, . 摘要:Gao, W.-C.; Tian, J., Science of Synthesis Knowledge Updates, (2020) 3, 292.