CAS: 98048-97-6; Fosinopril

该化合物是一种主要用于治疗高血压和心脏衰竭的抗抑制酶(ACE)抑制剂,其特点是能够抑制将血管一氧化乙酯转化为血管二氧化乙酯,这是一种强大的血管收缩器,因此可以促进血管扩张和减少血压.Fosinopril在ACE抑制剂中是独一无二的,因为它的双重消除途径,被排出异性与肝脏功能不同的病人.该物质通常以其抗药性的形式施用,这种药物在身体中转化为活性代谢.Fosinopril以相对较长的半衰期著称,允许一次一次性服用.常见的副作用可能包括咳嗽,高血糖和低温,与其他ACE抑制剂类似.其化学结构包括一种磷酸组,有助于其肾脏功能不同的病人.

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19H29O6PC19H29O6P trans-4-cyclohexyl-L-proline hydr°Chloride (2S,4S)-1-Benzoyl-4-phenyl-pyrrolidine-2-carboxylic acid trans-4-phenyl-L-proline

合成工艺路线路线简述

    反-4-苯基-L-脯氨酸置于吡啶,盐酸,5% Rhodium-On-Charcoal,氢气,三甲基乙酰氯,三乙胺体系中,用 甲醇,二氯甲烷 作为反应溶剂,-15.0~30.0 °C,2.0 Mpa 条件下,反应 8.0H,反应生成 福辛普利
    参考文献:一种降压药福辛普利钠及其关键中间体的制 备方法
    标题:一种降压药福辛普利钠及其关键中间体的制 备方法
    摘要:本发明涉及适用于工业化生产的一种降压药福辛普利钠及其关键中间体反式‑4‑苯基‑l‑脯氨酸的制备方法,其中关键中间体反式‑4‑苯基‑l‑脯氨酸的合成手性选择性高,方法简便易操作.

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-6717007-B1
    优先权日:1999-09-16
    标 题:Regiospecific synthesis of phosphonous acids
    发明人:DUBEY SUSHIL KUMAR; RAJGOPAL VENKAT; SINGH ANIL VIR; LAHIRI SASWATA; WANI MUKESH JAGANNATH
    权利人:LUPIN LTD
    摘要:An improved regiospecific synthesis of organic phosphonous acids, comprising of hydrophosphorylation of an olefin with hydrophosphorous acid in the presence of an inorganic persulfate, which acts as a source of free radicals at a pH ranging from 4.5 to 7.0, in which the orientation of addition is anti-Markonikoff. The process enables production of organic phosphonous acids at lower temperature and atmospheric pressure under milder pH conditions for better regioselectivity in hydrophosphorylation and obtain the phosphonous acid with good yield and purity following simple isolation procedure. Phosphonous acids obtained by the process are commercially valuable as effective detergents and wetting agents, lubricants and lubricant additives, plasticizers for plastics and resins, corrosion inhibitors, chemicals including insecticides and pesticides, cobalt extractants and as key intermediates for preparation of commercially important angiotensin converting enzyme (ACE) inhibitors.

    专利号:US-7582758-B2
    优先权日:2004-06-08
    标 题:Lewis acid mediated synthesis of cyclic esters
    发明人:MARTIN KEVIN V
    权利人:METABASIS THERAPEUTICS INC
    摘要:Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.

    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-5362899-A
    优先权日:1993-09-09
    标题:Chiral synthesis of alpha-aminophosponic acids
    发明人:CAMPBELL DAVID A
    权利人:AFFYMAX TECH NV
    摘要:A stereospecific method of preparing alpha-aminophosphonic acids and derivatives thereof is provided. A protected amino acid is converted to a acyl aroyl or diacyl peroxide which spontaneously rearranges to form an alpha-amino ester. This rearrangement occurs stereospecifically with retention of configuration. The ester is subsequently converted to an appropriate leaving group and displaced with a phosphite yielding a chiral alpha-aminophosphonic acid or derivative. n Alpha-aminophosphonic acids are useful for the synthesis of peptide analogs that possess a phosphonate linkage in the place of an amide linkage. This substitution can impart protease resistance in therapeutic peptides thereby increasing the serum half-life.
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    主要参考文献


    1: Xue K, Li G, Sun X, Hu Y, Hu L, Huang J, Si L. Simultaneous quantification of fosinopril and its active metabolite fosinoprilat in rat plasma by UFLC-MS/MS: Application of formic acid in the stabilization of an ester-containing drug. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 May 15;990:141-9. doi: 10.1016/j.jchromb.2015.03.028. Epub 2015 Apr 3. doi: 10.1007/s00210-014-1024-y. Epub 2014 Jul 27. doi: 10.1016/j.ejps.2013.12.009. Epub 2013 Dec 21. doi: 10.1007/s00210-014-0956-6. Epub 2014 Jan 19. doi: 10.1002/ddr.21280. Epub 2015 Sep 9. eCollection 2015.
    7: Green BR, Bain LJ. Mrp2 is involved in the efflux and disposition of fosinopril. J Appl Toxicol. 2013 Jun;33(6):458-65. doi: 10.1002/jat.1767. Epub 2011 Nov 17. doi: 10.1016/j.cellimm.2013.08.003. Epub 2013 Aug 20. doi: 10.1016/j.jpba.2014.01.010. Epub 2014 Jan 22. doi: 10.1155/2015/521718. Epub 2015 Aug 2.
    11: Zhang YC, Tang Y, Zhang M, Chen J, Zhou Q, Sun YG, Chen MT, Xu WP. Fosinopril attenuates the doxorubicin-induced cardiomyopathy by restoring the function of sarcoplasmic reticulum. Cell Biochem Biophys. 2012 Dec;64(3):205-11. doi: 10.1007/s12013-012-9386-6. Ukrainian. doi: 10.1093/jac/dks419. Epub 2012 Oct 30.

    合成参考文献


    摘要:Lednev OA, Zaslavskaia RM, Buniatian ND, Sergeev SV. [The use of monopril in elderly patients with arterial hypertension and coronary heart disease]. Klin Med (Mosk). 2009;87(12):48–9.
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