CAS: 3092-17-9; Midodrine Hydrochloride

该化合物是一种该化合物是一种选择性的α1-肾受体激动剂,由于血管抑制性能,它通常用于管理异体性弱化,通过增加外围血管抗药性,提高血压.该化合物的特点是可预测的药理动能,口服生物利用率和低血脑屏障渗透造成的微小中央...

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midodrine 2-azido-N-(β-hydroxy-2',5'-dimethoxyphenethyl)acetamide B°C-glycine desglymidodrine

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    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
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    合成参考文献


    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.
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