CAS: 76095-16-4; (S)-1-((S)-2-(((S)-1-Ethoxy-1-Oxo-4-Phenylbutan-2-yl)Amino)Propanoyl)Pyrrolidine-2-Carboxylic Acid Maleate

该化合物是一种主要用作高血压和心脏衰竭治疗抗血压剂的药物化合物,它是 enalapril 的酸衍生物,是一种抗血压和心脏衰竭的抑制酶(ACE) . 丁酸盐形式会增强药物的溶性性和稳定性. 乙酸丙烯酸盐通常是一种白色和非白晶状粉,其分子配方反映其复杂的结构,包括和阳性成分. 它在水和乙醇中溶解,但有机溶剂中的溶解性有限. 抑制乙酸乙酯酶的复合作用,导致乙酸乙酯的产量下降,导致血管变异和血压的降低. 常见的副作用包括眩晕,疲劳和咳,而严重的不良作用可能涉及肾脏损伤和高血糖. 乙酸雄性乙酸通常通过口授,并且通常与其他抗体固性药物相结合,以提高功效.

结构式图片

欧盟法规

C&L通报REACH预注册

上下游产品

CAS号110-16-7 马来酸 | CAS号147-85-3 脯氨酸 | CAS号75847-73-3 依那普利 | CAS号82717-96-2 N-[1-(S)-乙氧羰基-3... | CAS号103377-40-8 N-[1-(S)-ethoxy... | CAS号64920-29-2 2-氧代-基丁酸乙酯 | CAS号82009-36-7 N-[N-(1-(S)-eth... | CAS号2812-46-6 L-脯氨酸叔丁基酯 | CAS号80828-38-2 N-[(S)-1-(ethox... | CAS号76420-72-9 依那普利拉

合成工艺路线路线简述

  • 合成目标产物 Enalapril Maleate 主要起始原料 N-[(S)-(+)-1-(Ethoxycarbonyl)-3-Phenylpropyl]-L-Alanine
  • (文献来源)合成步骤主要原料 N-[(S)-(+)-1-(Ethoxycarbonyl)-3-Phenylpropyl]-L-Alanine

海关参考信息

专利信息


专利号:WO-2024213852-A1
优先权日:2023-04-12
标题:Electrochemical device for enzymatic synthesis of polynucleotides
发明人:HORGAN ADRIAN; FOURNIER MAXIME; GODRON XAVIER; BOUL MANON; CHEN SUYUE
权利人:DNA SCRIPT
摘要:The present invention relates to an electrochemical device (1) for enzymatic synthesis of polynucleotides, comprising at least one circulation duct (4) configured to receive an electrolytic solution, the circulation duct (4) being delimited by a first wall (6) and a second wall (7) opposite each other, the first wall (6) forming a support plate (8) of at least one reaction site configured for the enzymatic synthesis and able to carry a polynucleotide initiator fragment, the circulation duct (4) being equipped with a set of electrodes (2), the set of electrodes comprising at least one electrode of an array of electrodes (10) formed on the support plate (8) and operatively associated with the reaction sites, the set of electrodes (2) also comprising at least one additional electrode (16) arranged on the second wall (7) opposite the support plate (8).

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:WO-2024133119-A1
优先权日:2022-12-19
标 题:Process for the synthesis of isophorone in the liquid phase, including recycling of the by-products
发明人:RUPPIN CHRISTOPHE
权利人:ARKEMA FRANCE
摘要:The present invention relates to a continuous process for the synthesis of isophorone in the liquid phase by alkaline self-condensation of acetone, comprising the following successive steps: a) continuously injecting, through a tubular reactor (R), a stream of an aqueous alkali hydroxide solution and a stream of an organic solution comprising acetone and by-products recycled in step g), followed by b) condensation reaction of the acetone in the tubular reactor (R), then c) distillation of the reaction mixture from the tubular reactor (R), then d) separation of the concentrated raw reaction product from the distillation of step c), resulting in an alkaline aqueous phase and an organic phase containing isophorone, then e) distillation of the organic phase containing the isophorone recovered in the preceding step, then f) distillation of the polycondensation sub-products from the bottom of the column (D2) from the preceding distillation, then g) recycling, to the tubular reactor (R), of the stream from the column head of the preceding distillation (D3), said stream comprising xylitones and/or isoxylitones.

专利号:US-7094920-B2
优先权日:2001-05-21
标 题 :Stereoselective synthesis of 2-hydroxy-4-phenylbutyric acid esters
发明人:TIKARE RAVEENDRA KHANDURAO
权利人:FERMENTA BIOTECH LTD
摘要:A process is described for the stereospecific preparation of an ester of formula (I): wherein * signifies the (R) stereoisomer; R 1 is selected from C 1-6 alkyl, preferably ethyl; and R 2 is hydrogen, a protecting group or a leaving group which process comprises reaction of a nitrile of formula (II): wherein * signifies the (R) stereoisonomer; and Ph is the phenyl group C 6 H 5 with a solution of an inorganic acid in an alcohol and optional conversion of the compound of formula (I) wherein R 2 is H so prepared to any other desired compound of formula (I) by standard methods in the art. The compounds of formula (I) are chiral esters, useful as intermediates in the synthesis of the family of acetylcholine esterase (ACE) inhibitors known as “prilsâ€?, such as lisinopril, cilazapril, enalapril, benazepril, ramipril, delapril, enalaprilat, imidapril, spirapril, trandolapril and others.n n*n nPh-CH 2 —CH 2 —CH(OR 2 )—COOR 1   (I)n n*n nPh-CH 2 —CH 2 —CH(H)—CN  (II)

专利号:WO-2025068673-A1
优先权日:2023-09-29
标 题 :Process for the synthesis of methanol with optimised syngas preparation and processing
发明人:YIU KAR CHI
权利人:JOHNSON MATTHEY DAVY TECHNOLOGIES LTD
摘要:A process for synthesising methanol is described comprising the steps of (i) reforming a hydrocarbon feedstock in a hydrocarbon reforming unit comprising a fired heater and an autothermal reformer in series to form a synthesis gas containing hydrogen, carbon monoxide and carbon dioxide; (ii) dividing the synthesis gas into a first portion and a second portion, (iii) converting the first portion of synthesis gas into a methanol product in a methanol synthesis unit comprising one or more methanol synthesis reactors; and (iv) recovering a purge gas stream from the methanol synthesis unit, wherein the second portion of synthesis gas is passed to a hydrogen production unit where it is subjected to one or more stages of water gas shift in a water-gas shift unit to form a hydrogen-enriched gas, the a hydrogen-enriched gas is subjected to a step of carbon dioxide removal in a carbon dioxide removal unit to form a hydrogen product stream and a carbon dioxide stream, the carbon dioxide stream is recovered and at least a portion of the hydrogen product stream is fed to the fired heater as a fuel.

专利号:WO-2024009192-A3
优先权日:2022-07-06
标 题:Method of homolytic and heterolytic cleavage in molecules of gases and liquids
发明人:CHERNOV GENNADIY
权利人:DEREROY & CO A S
摘要:The method is for homolytic and heterolytic cleavage in molecules of gases and liquids with the release of bonding energy and its use to change the internal geometric architecture of some molecules, leading to the synthesis of new chemical compounds that are not contained in the initial gases and liquids, with the secondary release of energy during the synthesis process, without carrying out nuclear reactions on equipment for its realization, characterised by an increase in the energy of the work environment and use of this energy to generate thermal energy with simultaneous synthesis of new chemical compounds, in consequence of the physical effect of a standing pressure wave on the gas and liquid molecules at various temperatures, where the temperature is a measure of activation energy, and subsequent dissociation of the molecules into atoms or fragments of molecules (radicals), partial ionization of atoms and subsequent transformation of the bonds in atoms of the molecules with no change to atomic number but with a change to atomic mass and in the proton-neutron ratio. The method also consists in the direct conversion of neutron mass into the mass equivalent to the total mass of 1 electron and 1 proton that do not go beyond the framework of the electrodynamic interaction of electrons and the nucleus, which ensures the absence of radiation, where the method also consists in the transformation of an atom into a chemical molecule or the reverse transformation of 1 electron and 1 proton into 1 neutron from the volume, where these elementary particles can be free, with external exchange of energy and mass equalling the mass with a positive charge and equal to the reduction in the mass of the neutron and proton. The method furthermore consists in a back reaction to the physical effect consisting in the formation of new chemical compounds that are not contained in the initial gases and liquids, with the release of the energy produced during the process of recombination of atoms into the original molecules, where the execution of the proposed method takes place through a combination of initial influences, such as for example : 12 C 1 H 4 = 16 Ne = 16 O, while the method further consists in rearranging the architecture of some molecules without changing the atomic number, mass number, atomic weight as a reaction to a physical impact, during which new chemical compounds are synthesized, including those that they are not contained in the initial gases and liquids, while the energy generated during these synthesis reactions is released, for example 14 N 2 = 12 C 16 O; 12 C 16 O 2 = 14 N 2 16 O. The proposed method is implemented by a combination of initial influences, such as: • increase in temperature of up to 250°C, ideally 140°C to 150°C; • reduction in pressure (creation of a reduced atmosphere) to -100 kPa, ideally -65 kPa; • generation of standing pressure waves; • electric discharge (tribostatic discharge, barrier, spark) with a breakdown voltage of 1 to 15 kV; • the value of the magnetic field in the reactor based on the discharge in the gas is 70 to 120 nTI; • micro-explosions; • impact, impact force, at which negative acceleration at from 50,000 to 150,000 g occurs; • or a combination of these influences. The apparatus for converting hydrocarbon and non-hydrocarbon gases and liquids consists of • an acceleration module, which is a piece of apparatus accelerating a mixture of gas and liquid up to a speed of 30 to 400 m/s; • a deceleration module, which is a tribostatic energy generator covering 70% to 90% of the reactor's cross-section; • a tribostatic generator, which consists of two electrodes which are placed side by side an on which positive and negative charges are mutually created; • a reduced atmosphere zone after the deceleration module.
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主要参考文献


1: Aygen B, Kucuksu M, Aydin S, Ozercan IH. Effect of enalapril maleate on ghrelin levels in metabolic syndrome in rats. Peptides. 2015 May;67:39-44. doi: 10.1016/j.peptides.2015.03.002. Epub 2015 Mar 14. doi: 10.1016/j.ejps.2014.01.001. Epub 2014 Jan 20. doi: 10.1016/j.bbrc.2013.10.162. Epub 2013 Nov 8. doi: 10.2478/v10007-012-0039-5. doi: 10.3109/03639045.2011.589451. Epub 2011 Jul 1. doi: 10.4103/0250-474X.78522.
10: Toporisic R, Mlakar A, Hvala J, Prislan I, Zupancic-Kralj L. Identification of new impurities of enalapril maleate on oxidation in the presence of magnesium monoperoxyphthalate. J Pharm Biomed Anal. 2010 Jun 5;52(2):294-9. doi: 10.1016/j.jpba.2009.12.018. Epub 2009 Dec 29. doi: 10.1111/j.1755-3768.2008.01495.x. Epub 2009 Apr 29. English, Portuguese. Epub 2010 May 15.
14: Al-Arfaj NA, Al-Abdulkareem EA, Aly FA. Determination of enalapril maleate and atenolol in their pharmaceutical products and in biological fluids by flow-injection chemiluminescence. Luminescence. 2009 Nov-Dec;24(6):422-8. doi: 10.1002/bio.1129. Chinese. doi: 10.2460/ajvr.69.12.1574. doi: 10.1016/j.jpba.2008.02.030. Epub 2008 Mar 4. Chinese.

合成参考文献


参考文献:10.2165/00003495-199651050-00006
摘要:Wagstaff AJ, Davis R, McTavish D. Fosinopril: a reappraisal of its pharmacology and therapeutic efficacy in essential hypertension. Drugs. 1996 May;51(5):777–91. doi: 10.2165/00003495-199651050-00006.
参考文献:10.2165/00002018-199615010-00006
摘要:Overlack A. ACE inhibitor-induced cough and bronchospasm. Incidence, mechanisms and management. Drug Saf. 1996 Jul;15(1):72–8. doi: 10.2165/00002018-199615010-00006.
参考文献:10.1007/bf02627955
摘要:Byyny RL, Merrill DD, Bradstreet TE, Sweet CS. An inpatient trial of the safety and efficacy of losartan compared with placebo and enalapril in patients with essential hypertension. Cardiovasc Drugs Ther. 1996 Jul;10(3):313–9. doi: 10.1007/bf02627955.
参考文献:10.1007/s002280050158
摘要:Ajayi AA, Afolabi MA, Balogun MO, Adigun AQ, Ajayi OE, Akintomide AO. Oral therapy with combined enalapril, prazosin and hydrochlorothiazide in the acute treatment of severe hypertension in Nigerians. European Journal of Clinical Pharmacology. 1996 Sep 02;51(1):45–8. doi: 10.1007/s002280050158.
参考文献:10.1007/s11033-012-2468-0
摘要:Tang LQ, Wang FL, Zhu LN, Lv F, Liu S, Zhang ST. Berberine ameliorates renal injury by regulating G proteins-AC- cAMP signaling in diabetic rats with nephropathy. Molecular Biology Reports. 2012 Dec 25;40(6):3913–23. doi: 10.1007/s11033-012-2468-0.
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