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: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
专利号:WO-0179154-A2 优先权日:2000-04-17 标 题:Synthesis of midodrine hci from a novel intermediate 1-(2',5'-dimethoxyphenyl)-2-azidoethanone
摘要:Drugs in Japan, -(1152), 1990 摘要:Archives Internationales de Pharmacodynamie et de Therapie., 247(217), 1980 [] 参考文献:10.1007/s11886-004-0042-7 摘要:Melby DP, Cytron JA, Benditt DG. New approaches to the treatment and prevention of neurally mediated reflex (neurocardiogenic) syncope. Curr Cardiol Rep. 2004 Sep;6(5):385–90. doi: 10.1007/s11886-004-0042-7.