CAS: 81872-10-8; Zofenopril

该化合物是主要用于管理高血压和心脏衰竭的抗抑制酶(ACE),其主要优点包括:硫化氢酶,它能增加组织渗透,延长其行动时间,而与其他ACE抑制剂相比,它能增加组织渗透,延长行动时间.Zofenopril被代谢为其活性形式,Zofenopril, 表现出强大的血管和心血管保护效应.临床研究已经证明它能有效降低血压,改善内宫功能,并具有有利的安全特征.此外,它的亲食性能有助于改善细胞吸收,使其在心血管炎患者中特别有效.该药物经常每天服用一次,改善患者的合规性.

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物理性质

MSDS等安全信息

上下游产品

CAS号105107-84-4 (4S)-4-(苯硫基)-L-... | CAS号74654-91-4 S-benzoyl-3-mer... | CAS号81938-38-7 (4S)-1((2S)-3-(... | CAS号81653-77-2 Cis-4-phenylthi... | CAS号81938-43-4 佐芬普利钙

合成工艺路线路线简述

  • 合成目标产物 Zofenopril 主要起始原料 Cis-4-Phenylthio-L-Proline Hydrochloride And S-Benzoyl-3-Mercapto-2-Methylpropanoyl Chloride
  • 72679-02-8 = 81872-10-8
    反应条件:1.1 Reagents: Thionyl Chloride; 1 H,Rt; Reflux -> 70 °C; 5 H,60 - 70 °C2.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C2.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C2.3 Reagents: Ethyl Acetate; 4 H2.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China]

    947611-60-1 = 81872-10-8
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; 4 H,Reflux; Overnight,Rt2.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C2.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C2.3 Reagents: Ethyl Acetate; 4 H2.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China]

    = 81872-10-8
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Ethanol; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 22.1 Reagents: Hydrochloric Acid Solvents: Water; 4 H,Reflux; Overnight,Rt3.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C3.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C3.3 Reagents: Ethyl Acetate; 4 H3.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China]

    67943-19-5 = 81872-10-8
    反应条件:1.1 Solvents: Pyridine; 30 Min,0 - 10 °C2.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 1 H,Cooled2.2 Overnight,Rt3.1 Reagents: Sodium Hydroxide Solvents: Ethanol; Overnight,Rt3.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 24.1 Reagents: Hydrochloric Acid Solvents: Water; 4 H,Reflux; Overnight,Rt5.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C5.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C5.3 Reagents: Ethyl Acetate; 4 H5.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China]

    105107-84-4 + 74654-91-4 = 81872-10-8
    反应条件:1.1 Reagents: Sodium Bicarbonate,Sodium Carbonate Solvents: Acetone,Water; Ph 8 - 10,15 - 20 °C; 20 °C -> Rt; 3 H,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2
    标题:An Improved Large Scale Procedure For The Preparation Of N-Cbz Amino Acids
    作者:Pehere,Ashok D.; Et Al
    参考文献:Tetrahedron Letters 日期:2011 卷标:52(13) 页码:1493-1494]

    105107-84-4 + 72679-01-7 = 81872-10-8
    反应条件:1.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C1.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C1.3 Reagents: Ethyl Acetate; 4 H1.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China]

    72679-02-8 = 81872-10-8
    反应条件:1.1 Reagents: Thionyl Chloride Solvents: Toluene2.1 Reagents: Sodium Bicarbonate,Sodium Carbonate Solvents: Acetone,Water; Ph 8 - 10,15 - 20 °C; 20 °C -> Rt; 3 H,Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2
    标题:An Improved Large Scale Procedure For The Preparation Of N-Cbz Amino Acids
    作者:Pehere,Ashok D.; Et Al
    参考文献:Tetrahedron Letters 日期:2011 卷标:52(13) 页码:1493-1494]

    57750-51-3 = 81872-10-8
    反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 1 H,Cooled1.2 Overnight,Rt2.1 Reagents: Sodium Hydroxide Solvents: Ethanol; Overnight,Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 23.1 Reagents: Hydrochloric Acid Solvents: Water; 4 H,Reflux; Overnight,Rt4.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C4.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C4.3 Reagents: Ethyl Acetate; 4 H4.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China]

    33996-33-7 = 81872-10-8
    反应条件:1.1 Catalysts: P-Toluenesulfonic Acid Solvents: Methanol; 45 Min,Rt; 48 H,Rt1.2 Reagents: Sodium Bicarbonate Solvents: Water; Ph 72.1 Solvents: Pyridine; 30 Min,0 - 10 °C3.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 1 H,Cooled3.2 Overnight,Rt4.1 Reagents: Sodium Hydroxide Solvents: Ethanol; Overnight,Rt4.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 25.1 Reagents: Hydrochloric Acid Solvents: Water; 4 H,Reflux; Overnight,Rt6.1 Reagents: Sodium Carbonate Solvents: Water; Ph 8 - 9,0 - 10 °C6.2 Reagents: Sodium Carbonate Solvents: Water; 1.5 - 2 H,Ph 8 - 9,0 - 10 °C6.3 Reagents: Ethyl Acetate; 4 H6.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 - 2
    标题:Improved Method For Synthesizing Zofenopril Calcium From N-Acetyl-L-Hydroxyproline
    参考文献:China
📜佐芬普利叔丁胺盐置于盐酸体系中,用 二氯甲烷,水 作为反应溶剂,化学反应 0.5H,反应生成 佐芬普利
参考文献: A Process For The Preparation Of Zofenopril And Its Pharmaceutically Acceptable Salts Thereof[fr] Procédé Pour La Préparation De Zofénopril Et Ses Sels Pharmaceutiquement Acceptables
标题: A Process For The Preparation Of Zofenopril And Its Pharmaceutically Acceptable Salts Thereof[fr] Procédé Pour La Préparation De Zofénopril Et Ses Sels Pharmaceutiquement Acceptables

海关参考信息

专利信息


专利号:US-8431712-B2
优先权日:2004-02-09
标 题 :Methods for the synthesis of pyridoxamine
发明人：KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT
权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC
摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, 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 compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide 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 pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-7708989-B2
优先权日:1999-10-29
标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
发明人：LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
权利人:NITROMED INC
摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.

专利号:US-7384976-B2
优先权日:2001-05-02
标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
发明人：GARVEY DAVID S
权利人:NITROMED INC
摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

专利号:US-2008090885-A1
优先权日:2006-10-12
标题:Preparation of losartan 5-carboxylic acid and use thereof
发明人：CHEN LIQIN; LI JIAN; SHEN YINGZHONG
权利人:CHEN LIQIN; LI JIAN; SHEN YINGZHONG
摘要:A method for synthesis of losartan 5-carboxylic acid (EXP-3174).

专利号:US-2011281928-A1
优先权日:2009-01-23
标 题:Process for the preparation of zofenopril and its pharmaceutically acceptable salts thereof
发明人：KHAN MUBEEN AHMED; YADAV ROOP SINGH; TRIVEDI NIKHIL RASIKLAL; LAD SACHIN MAHEDO
权利人:KHAN MUBEEN AHMED; YADAV ROOP SINGH; TRIVEDI NIKHIL RASIKLAL; LAD SACHIN MAHEDO; GLENMARK GENERICS LTD
摘要:The present invention relates to a process for the preparation of zofenopril and its pharmaceutically acceptable salts and a pharmaceutical composition thereof. The present invention also provides structurally novel compounds, which are useful intermediates in the synthesis of zofenopril.

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合成参考文献


摘要:Abuladze GV, Nebieridze MI, Narsiia EV, Erkomaishvili IG, Pipiia NG. [Efficiancy Angiotensin -converting enzyme inhibitors for the clinical practice]. Georgian Med News. 2011 Jun;(195):37–40.
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