CAS: 103890-78-4; (E)-Diethyl 4-(2-(3-(Tert-Butoxy)-3-Oxoprop-1-En-1-yl)Phenyl)-2,6-Dimethyl-1,4-Dihydropyridine-3,5-Dicarboxylate

该化合物是一种主要用作抗血压剂的钙管阻塞剂,它属于二氢类化合物,具有选择性抑制L型钙管的能力,导致血管变异,导致血压下降,其分子结构包括二氢,这是其药理活动所必不可少的.它以其长的半衰期而著称,允许一次日服,这可以加强病人的合规性.酸性表现出脂性能,方便其吸收和在体内分布.此外,它具有潜在的抗氧化效应,可能会促进其心血管作用,而这种效应不仅会减少血压.该物质通常以平板形式施用,而且可能会产生副作用,例如边缘的乳房或冲水,尽管一般都受到很好的调适.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号59159-39-6 (叔丁氧基羰基甲基)三苯基溴化鏻 | CAS号626-34-6 3-氨基巴豆酸乙酯 | CAS号643-79-8 邻苯二甲醛 | CAS号103890-69-3 3-(2-甲酰基苯基)-2-(... | CAS号144-55-8 碳酸氢钠

合成工艺路线路线简述

  • 合成目标产物 Lacidipine 主要起始原料 (Tert-Butoxycarbonylmethyl)Triphenylphosphanium Bromide And Ethyl 3-Aminocrotonate And O-Phthalaldehyde
  • (文献来源)合成步骤主要原料 (Tert-Butoxycarbonylmethyl)Triphenylphosphanium Bromide 和 Ethyl 3-Aminocrotonate 和 O-Phthalaldehyde
3-(2-甲酰基苯基)-2-(E)-丙烯酸叔丁酯,(E)-3-氨基巴豆酸乙酯 反应生成拉西地平
参考文献:Semeraro,Claudio;Micheli,Dino;Pieraccioli,Daniele;Gaviraghi,Giovanni;+
标题:Semeraro,Claudio;Micheli,Dino;Pieraccioli,Daniele;Gaviraghi,Giovanni;+

专利信息


专利号:US-9440928-B2
优先权日:2011-07-20
标题 :Process for the synthesis of N-substituted cyclic alkylene ureas
发明人:GUPTA RAM; KOBYLANSKA IRINA; TREASURER URVEE; FLOOD LAWRENCE
权利人:GUPTA RAM; KOBYLANSKA IRINA; TREASURER URVEE; FLOOD LAWRENCE; ALLNEX IP S AR L
摘要:The invention relates to a process for the synthesis of N-substituted cyclic alkylene ureas by reacting a multifunctional aliphatic amine A having at least two amino groups which may be primary or secondary, at least one of which is a primary amino group, —NH 2 , and at least one of which is a secondary amino group, >NH, the other hydrogen group whereof having been substituted by a hydrocarbyl group which in turn may be substituted by a hydroxyl group, or an amino group, or a carboxyl group, or a ketone carbonyl group, or a hydrazide or hydrazone group, or a mercaptan group, and at least one further functional group selected from the group consisting of primary or secondary amino groups and hydroxyl groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA.

专利号:US-5491245-A
优先权日:1993-03-26
标 题 :Method for the synthesis of amphoteric surfactants
发明人:GRUENING BURGHARD; WEITEMEYER CHRISTIAN
权利人:GOLDSCHMIDT AG TH
摘要:A method for the synthesis of amphoteric surfactants by the reaction of amines with chloroacetic acid or its salts in aqueous solution at an elevated temperature, consists of reacting compounds of the general formula ##STR1## with chloroacetic acid at temperatures ranging from 115° to 180° C., until the chloroacetic acid content is less than 10 ppm.

专利号:US-4472568-A
优先权日:1981-11-12
标 题:Process for the preparation of polyamines from N-monoaryl-N',N'-dialkyl urea compounds and their use for the synthesis of polyurethanes
发明人:RASSHOFER WERNER; GROEGLER GERHARD
权利人:BAYER AG
摘要:This invention relates to an improved process for the preparation of aromatic polyamines containing urethane and/or biuret and/or urea and/or isocyanurate groups and preferably also ether groups by the hydrolysis of poly-N-monoaryl-N',N'-dialkyl urea compounds (1-aryl-3,3-dialkyl ureas). The ureas are obtained by the reaction of secondary aliphatic, cycloaliphatic or saturated heterocyclic amines with divalent to tetravalent isocyanate compounds containing isocyanate end groups attached to aromatic residues. The ureas correspond to the general formula: wherein R1, R2 denote alkyl or cycloalkyl groups, or together form a ring and A denotes a divalent to tetravalent residue attached to the ureas by aromatic groups. Hydrolysis is carried out in the presence of water and up to two equivalents of a base containing hydroxide ions and/or up to two equivalents of a compound containing tertiary amino groups, optionally in the presence of solvents. The use of the polyamines obtained by this process for the synthesis of polyurethanes is also described.

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:EP-3967330-A1
优先权日:2020-09-10
标 题:Methods for the synthesis of bioactivated metal nanocluster and their medical application
发明人:MARCHI VALÉRIE; CHIECHIO REGINA MARIA; EVEN-HERNANDEZ PASCALE
权利人:UNIV RENNES; CENTRE NAT RECH SCIENT; INSTITUT NAT DES SCIENCES APPLIQUEES DE RENNES; ECOLE NAT SUPERIEURE DE CHIMIE DE RENNES
摘要:The present invention relates to a bioactivated metal nanocluster comprising a mixture of ligands linked to a fluorescent metallic nanocluster, their synthesis methods, and their medical applications.
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主要参考文献

1. Micheli, D., Collodel, A., Semeraro, C., et al. Lacidipine: A calcium antagonist with potent and long-lasting antihypertensive effects in animal studies. J. Cardiovasc. Parmacol. 15(4), 666-675 (1990). 2. Lupo, E., Locher, R., Weisser, B., et al. In vitro antioxidant activity of calcium antagonists against LDL oxidation compared with α-tocopherol. Biochem. Biophys. Res. Commun. 203(3), 1803-1808 (1994). 3. Kyselovic, J., Martinka, P., Batova, Z., et al. Calcium channel blocker inhibits Western-type diet-evoked atherosclerosis development in ApoE-deficient mice. J. Pharmacol. Exp. Ther. 315(1), 320-328 (2005).

合成参考文献


参考文献:10.1097/00005344-199608000-00021
摘要:Lau C, Cheung BMY. Relative Efficacy and Tolerability of Lacidipine and Amlodipine in Patients with Mild-to-Moderate Hypertension: A Randomized Double-Blind Study. Journal of Cardiovascular Pharmacology. 1996 Aug;28(2):328–31. doi: 10.1097/00005344-199608000-00021.
参考文献:10.2165/00002018-199615030-00007
摘要:Brunet L, Miranda J, Farré M, Berini L, Mendieta C. Gingival enlargement induced by drugs. Drug Saf. 1996 Sep;15(3):219–31. doi: 10.2165/00002018-199615030-00007.
参考文献:10.2165/00002018-199615020-00002
摘要:Dougall HT, McLay J. A comparative review of the adverse effects of calcium antagonists. Drug Saf. 1996 Aug;15(2):91–106. doi: 10.2165/00002018-199615020-00002.
参考文献:10.1007/s00059-004-2550-z
摘要:Scholze J. [Pulse pressure in the therapeutic management of hypertension ]. Herz. 2004 May;29(3):276–89. doi: 10.1007/s00059-004-2550-z.
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