米多君置于盐酸体系中,用 乙醇,异丙醇 作为反应溶剂,以96%的收率获得产物2-氨基-N-[2-(2,5-二甲氧基苯基)-2-羟基乙基]乙酰胺盐酸盐 参考文献:A Process For The Preparation Of Midodrine 标题:A Process For The Preparation Of Midodrine
专利号:US-7094928-B2 优先权日:2002-08-21 标题 :Process for the synthesis of (±) 2-Amino-N-[2,(2,5-dimethoxy phenyl)-2-hydroxyethyl] acetamide monohydrochloride 发明人:SUBRAMANIAN RAJARAM SANKARA; SATAGOPAN VENKATANATHAN; SRINIVASAN RAJAGOPALAN 权利人:SANMAR SPECIALTY CHEMICALS LTD 摘要:This invention relates to an improved process for synthesizing (±)-2-Amino-N-[2-(2,5-dimethoxyphenyl]-2-hydroxyethyl acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5-dimethoxyphenyl)-2-bromoethanone by reacting the same with hexamine in the presence of novel solvent system comprising Tetrahydrofuran and water. The resulting aminoethanone is acylated with haloacetylchloride and sodium acetate in acetone-water solvent system. This product is reduced selectively first with sodium borohydride and subsequently with stannous chloride. This product is converted in situ to the corresponding hydrochloride salt immediately after reduction on its own.
专利号:US-6201153-B1 优先权日:2000-04-17 标 题 :Synthesis of midodrine HCI from a novel intermediate 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone 发明人:RAY ANUP K; PATEL HIREN; PATEL MAHENDRA R 权利人:GENEVA PHARMACEUTICALS INC 摘要:Midodrine hydrochloride, ±1-(2',5'-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2',5'-dimethoxyphenyl)-2-azidoethanone.
专利号:EP-1276711-A2 优先权日:2000-04-17 标 题 :Synthesis of midodrine hci from a novel intermediate 1-(2',5'-dimethoxyphenyl)-2-azidoethanone
专利号:AU-2001258344-A1 优先权日:2000-04-17 标题:Synthesis of midodrine hci from a novel intermediate 1-(2',5'-dimethoxyphenyl)-2-azidoethanone
专利号:US-2004198836-A1 优先权日:2002-08-21 标 题:Process for the synthesis of (+) 2-amino-n-{2, (2,5-dimethoxy phenyl)-2-hydroxyethyl} acetamide monohydrochloride
专利号:EP-1465860-A1 优先权日:2002-08-21 标 题:An improved process for the synthesis of ( ) 2-amino-n-[2,(s,5-dimethoxyphenyl)-2-hydroxyethyl] acetamide monohydrochloride
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