2-甲氧基-5-(2-氧代丙基)苯磺酰氯置于ammonium Hydroxide体系中,用 四氢呋喃 用作溶剂,化学反应 2.0H,反应生成5-丙酮基-2-甲氧基苯磺酰胺 参考文献:Novel Phenoxyalkylamine Derivatives. Vii. Synthesis And Pharmacological Activities Of 2-Alkoxy-5-((Phenoxyalkylamino)Alkyl)Benzenesulfonamide Derivatives. 标题:Novel Phenoxyalkylamine Derivatives. Vii. Synthesis And Pharmacological Activities Of 2-Alkoxy-5-((Phenoxyalkylamino)Alkyl)Benzenesulfonamide Derivatives. 摘要:为了找到一种对多巴胺d2受体亲和力具有高选择性的新的α-拮抗剂,我们对2-烷氧基-5-[(苯氧烷基氨基)烷基]苯磺酰胺衍生物的烷基链及两个苯环上的取代基进行了结构改造.发现位于分子中心的氨基部分与苯环(环a)之间的烷基链的改造是最显著的.具备1-甲基乙基作为烷基链的5-[2-[[2-(5-氟-2-甲氧基苯氧基)乙基]氨基]丙基]-2-甲氧基苯磺酰胺(ii-4)表现出高α-拮抗选择性以及强效的α-拮抗活性. Doi:10.1248/cpb.40.1443
专利号:WO-2012101648-A1 优先权日:2011-01-24 标题:Novel process for the synthesis of enantiomerically pure 2-methoxy-5-[(2r)-2-(4-alkylpiperazin-l-yl)propyl]-benzenesulfonamide 发明人:HAVALDAR FREDDY H; DABHOLKAR BHUSHAN VASANT; MULE GANESH BABAN 权利人:HAVALDAR FREDDY H 摘要:Where R is C1-C3 alkyl, alkenyl A novel process for synthesis of compound of Formula 1 comprising steroselective catalytic reduction of compound of Formula IV under hydrogen gas pressure to obtain an intermediate compound of Formula II, which on coupling in presence of coupling agent and base in presence of organic solvent to obtain compound of Formula X, Formula X on reacting with deprotecting agent in presence of organic solvent results in formation of compound of Formula XI, condensation of Formula XI with alkyl halide results in formation of compound of Formula I.
专利号:US-7538246-B2 优先权日:2003-12-29 标 题:Synthesis of optically pure(r)-5-(2-amynopropyl)-2-methoxybenzenesulphonamide 发明人:MOHAR BARBARA 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to a new process for the preparation of optically pure(R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide, which is an intermediate in the synthesis of tamsulosin.
专利号:WO-2007104357-A1 优先权日:2006-03-14 标 题 :Synthesis of amines with catalytic amounts of mild lewis acids 发明人:NUGENT THOMAS CHRISTOPHER; WAKCHAURE VIJAY NARAYAN; EL-SHAZLY MOHAMED MAHMOUD 权利人:UNIV JACOBS BREMEN GMBH; NUGENT THOMAS CHRISTOPHER; WAKCHAURE VIJAY NARAYAN; EL-SHAZLY MOHAMED MAHMOUD 摘要:The invention relates to methods for producing primary, secondary and tertiary amines and corresponding enantiopure or enantioenriched primary or secondary amine products, comprising the steps of reductively aminating a ketone, with a nitrogen auxiliary in the presence of a hydrogenating catalyst and a hydrogenating agent, wherein the reductive animation is performed under the influence of a mild Lewis acid, the mild Lewis acid being present at the onset of the reductive amination in at most 25 mol% of the ketone or the nitrogen auxiliary.
专利号:US-2006148046-A1 优先权日:2004-12-31 标题 :Enzymatic process for the preparation of an intermediate compound and use thereof for the synthesis of tamsulosin hydrochloride
专利号:US-2007155989-A1 优先权日:2003-12-29 标 题 :Synthesis of optically pure(r)-5-(2-amynopropyl)-2-methoxybenzenesulphonamide
专利号:AU-2004309314-B2 优先权日:2003-12-29 标题 :Synthesis of optically pure (R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide
参考标题: Novel Process For The Synthesis Of Enantiomerically Pure 2-Methoxy-5-[(2R)-2-(4-Alkylpiperazin-L-Yl)Propyl]-Benzenesulfonamide Nouveau Procédé De Synthèse De 2-Méthoxy-5-[(2R)-2-(4-Alkylpipérazin-L-Yl)Propyl]-Benzènesulfonamide énantiomériquement Pur 摘要:Where R Is C1-C3 Alkyl, Alkenyl A Novel Process For Synthesis Of Compound Of Formula 1 Comprising Steroselective Catalytic Reduction Of Compound Of Formula Iv Under Hydrogen Gas Pressure To Obtain An Intermediate Compound Of Formula Ii, Which On Coupling In Presence Of Coupling Agent And Base In Presence Of Organic Solvent To Obtain Compound Of Formula X, Formula X On Reacting With Deprotecting Agent In Presence Of Organic Solvent Results In Formation Of Compound Of Formula Xi, Condensation Of Formula Xi With Alkyl Halide Results In Formation Of Compound Of Formula I.