专利号:US-3839325-A 优先权日:1973-03-23 标题:Synthesis of 4-sulfonamidophenyl hydrazines 发明人:HOFFSTADT W 权利人:GAF CORP 摘要:A synthesis is disclosed utilizing p-chlorobenzene-sulfonamide compounds of the following formula: IN WHICH R and R1 independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl, alkaryl, aralkyl or aryl, which may or may not be further substituted, or together with the nitrogen atom form a heterocyclic ring. These compounds are dissolved in dimethyl sulfoxide (DMSO), mixed with aqueous hydrazine hydrate and heated until completely reacted to form 4 - sulfonamidophenyl hydrazines that can be readily separated from the reaction media by precipitation with water. The precipitate can be readily washed and dried to provide a pure, substituted sulfonamido hydrazine. The product is obtained in high yields frequently of about 80 - 90 percent and is sufficiently pure for subsequent use in the preparation of substituted phenyl pyrazolones which in turn are useful as magenta color formers in color photography. For example, p-chloro-benzene-sulfonyl morpholine is dissolved in DMSO and reacted under reflux conditions with aqueous hydrazine hydrate to form 4 - morpholino - sulfonamido-phenyl hydrazine having a melting point of 162*- 164*C after purification.
专利号:US-2011137040-A1 优先权日:2008-08-01 标 题 :Synthesis of 3,4-diaryl-4,5-dihydro-(h)-pyrazole-1-carboxamidine derivatives 发明人:LANGE JOSEPHUS H M; SANDERS HANS J; RHEENEN JEROEN VAN 权利人:LANGE JOSEPHUS H M; SANDERS HANS J; RHEENEN JEROEN VAN 摘要:The invention relates to a novel chemical route to 3,4-diaryl-4,5-dihydro-(1H)-pyrazole-1-carbox-amidine derivatives, known as potent cannabinoid-CB 1 receptor antagonists, and to novel intermediates of these compounds. The synthetic route produced considerably higher yields than those reported, without the use of corrosive reagents. The process concerns the preparation of a compound of formula (I): n n n n n n n n n n wherein the symbols have the meanings given in the description.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel 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 at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, 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 and/or respiratory toxicity; 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-2023266302-A1 优先权日:2020-07-24 标 题:Synthesis and use of n-benzyl sulfonamides 发明人:LAMAR ANGUS A; SHEAFF ROBERT J 权利人:THE UNIV OF TULSA 摘要:Disclosed is a method for preparing N-benzyl sulfonamides. Also disclosed is a composition for treating cancer. The composition includes a N-benzyl sulfonamide and a metabolic inhibitor. Also disclosed is a method for determining the impact on cell ATP levels of a composition containing a N-benzyl sulfonamide with or without a metabolic inhibitor.
专利号:US-7087783-B2 优先权日:2000-05-29 标 题 :Method for preparing nitrogen-containing compounds 发明人:EMURA TAKASHI; HANEISHI TSUYOSHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitriles or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.
专利号:US-7495108-B2 优先权日:2004-02-19 标 题:Imidazoline derivatives having CB1-antagonistic activity 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; VAN STUIVENBERG HERMAN H 权利人:SOLVAY PHARM BV 摘要:The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) n nwherein the symbols have the meanings given in the specification.
1: Rehman A, Abbasi MA, Siddiqui SZ, Mohyuddin A, Nadeem S, Shah SA. Synthesis, spectral analysis and biological evaluation of Nalkyl/aralkyl/aryl-4-chlorobenzenesulfonamide derivatives. Pak J Pharm Sci. 2016 Sep;29(5):1489-1496. doi: 10.7150/thno.15257. eCollection 2016. 3: Kim KY, Cho HS, Lee SH, Ahn JH, Cheon HG. Neuroprotective effects of KR-62980, a new PPARγ agonist, against chemical ischemia-reperfusion in SK-N-SH cells. Brain Res. 2011 Feb 4;1372:103-14. doi: 10.1016/j.brainres.2010.11.062. Epub 2010 Nov 25. doi: 10.1016/j.bmcl.2010.06.085. Epub 2010 Jun 19. Epub 2006 Jun 14.
合成参考文献
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