CAS: 63675-72-9; 3-Isobutyl 5-Methyl 2,6-Dimethyl-4-(2-Nitrophenyl)-1,4-Dihydropyridine-3,5-Dicarboxylate

该化合物是主要用于治疗高血压和皮质的钙管阻塞剂,属于二氢正丙里丁类的钙对抗者,它通过L型钙渠道阻塞在血管滑动肌肉和心脏组织中通过L型钙化离子流入,导致血管通气和血压消减.尼索尔德皮ine的特征是其亲脂性,它加强了体内的吸收和分布.该化合物通常具有很长的半衰期,允许一次性服用.其化学结构包括一种对其药理活动至关重要的二氢丙里丁环.尼索尔迪平物质一般都受到很好的调制,但与其他钙气管阻塞剂一样,它可能会产生副作用,如外溢血肿,头痛和冲浪等.重要的是监测病人与其他药物的潜在相互作用,以及评估治疗期间的肾和肝功能.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

CAS号61312-59-2 Isobutyl 2-(2-N... | CAS号21731-17-9 β-氨基巴豆酸甲酯 | CAS号21829-25-4 硝苯地平 | CAS号55985-32-5 尼卡地平 | CAS号103026-83-1 Dehydro Nisoldipine

合成工艺路线路线简述

  • 合成目标产物 Nisoldipine 主要起始原料 Isobutyl 2-(2-Nitro-Benzylidene)Acetoacetate And Methyl 3-Aminocrotonate
  • (文献来源)合成步骤主要原料 Isobutyl 2-(2-Nitro-Benzylidene)Acetoacetate 和 Methyl 3-Aminocrotonate
2-[(2-硝基苯基)亚甲基]-3-氧代丁酸异丁酯,3-氨基巴豆酸甲酯 反应 0.15H,反应生成 尼索地平
参考文献:一种有效的和可回收的三维印刷的α-Al 2 ö 3催化剂对于该多组分生物活性组件的杂环
标题:一种有效的和可回收的三维印刷的α-Al 2 ö 3催化剂对于该多组分生物活性组件的杂环
摘要:报道了一种催化方法,该方法能够有效,操作简单且环保地合成各种1,4-二氢吡啶和3,4-二氢嘧啶-2(1 H)-One,包括一些相关药物和药理活性衍生物.该策略基于使用3D打印的al 2 O 3木桩材料,该材料经过烧结以产生具有受控孔隙率和显着催化性能的刚性结构.3D打印的al 2 O 3催化剂在biginelli和hantzsch反应中显示出路易斯酸的显着功效,并且可以回收并重复使用十次而不会降低活性.卓越的e 因素,出色的可回收性和可扩展性,广泛的底物范围,短的反应时间,优异的产率,无溶剂条件和易于分离的程序是该方法的关键特征.
DOI:10.1016/j.Apcata.2016.11.031

海关参考信息

专利信息


专利号:WO-2011130852-A1
优先权日:2010-04-21
标题:Preparation of intermediates for the synthesis of dihydropyridine calcium channel blockers
发明人:SOUZA FABIO; PAN MING
权利人:ALPHORA RES INC; SOUZA FABIO; PAN MING
摘要:4- (2,3- dichlorophenyl) -1,4- dihydro- 2,6- dimethyl- 5- methoxycarbonyl- 3- pyridinecarboxylic acid, a key intermediate in the synthesis of the cardiovascular calcium channel blocker drug 3-butanoyloxymethoxycarbonyl-5- methoxycarbonyl-4- (2,3-dichlorophenyl) -2,6- dimethyl-1,4- dihydropyridine, of purity greater than 97% and essentially free of the corresponding diacid, is prepared by a process involving selective precipitation of its carboxylate via addition of concentrated solutions of alkali metal salts. Similar intermediate mono-carboxylic acids useful in the synthesis of other unsymmetrically substituted dihydropyrine drugs such as nisoldipine, nitrendipine and nimodipine can be similarly prepared and purified.

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-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: White WB. Pharmacologic agents in the management of hypertension--nisoldipine coat-core. J Clin Hypertens (Greenwich). 2007 Apr;9(4):259-66. Review. Review. Review. Erratum in: Clin Pharmacokinet 1998 Nov;35(5):390. Review. Review. Review. Review. Review. Review. Review. Review. German. Review. Review. Review. Review. Review. Review. Review. Review. Russian. Review.

合成参考文献


参考文献:10.1007/s00210-011-0664-4
摘要:Goegelein H, Gautier P, Roccon A, O'Connor S, Ruetten H. Effects of the novel amiodarone-like compound SAR114646A on cardiac ion channels and ventricular arrhythmias in rats. Naunyn Schmiedebergs Arch Pharmacol. 2011 Sep;384(3):231–44. doi: 10.1007/s00210-011-0664-4.
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