CAS: 75695-93-1; 3-Isopropyl 5-Methyl 4-(Benzo[c][1,2,5]Oxadiazol-4-yl)-2,6-Dimethyl-1,4-Dihydropyridine-3,5-Dicarboxylate

该化合物是一种主要用于治疗高血压和腹膜切除的二氢钙管阻塞器,通过选择性抑制L型钙管发挥作用,导致血管变异和边缘血管抗药性减少; 甲状腺的特点是能够降低血压,但不会显著影响心率; 化合物通常通过口服施用,其半衰期相对较长,允许每天服药一两次; 其化学结构包括一种二氢环,这是其药理活动必不可少的; 与其它抗血压剂相比,甲状腺线具有有利的副作用,尽管它仍可能造成周围的血肿,眩晕或一些病人的冲水; 该物质主要通过细胞色素P450酶在肝脏中发生代谢,主要在尿液中被排出.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

2-acetyl-3-benzofurazan-4-yl-acrylic acid methyl ester isopropyl 3-amin°Crotonate(+)-PN 200-110 (-)-(R)-isradipine

合成工艺路线路线简述

    2-Acetyl-3-Benzofurazan-4-Yl-Acrylic Acid Methyl Ester,尼莫地平杂质3 以 乙醇 作为反应溶剂,化学反应 7.0H,反应生成 伊拉地平
    参考文献: An Improved Process For The Manufacture Of Isradipine.[fr] Procede Ameliore De Fabrication D'Isradipine
    标题: An Improved Process For The Manufacture Of Isradipine.[fr] Procede Ameliore De Fabrication D'Isradipine
    摘要:该发明涉及一种改进的异拉地平(isradipine)制备方法,包括在异丙醚中,在乙酸和哌啶的存在下,将2,1,3-苯并噻二唑-4-甲醛与乙酰乙酸甲酯反应.从而得到2-乙酰-3-苯并呋噻-4-基丙烯酸甲酯产物,然后将其与乙醇中的异丙基-ß-氨基丙烯酸酯在25至35oc反应以获得产物.

    海关参考信息

    专利信息


    专利号:US-2010143980-A1
    优先权日:2007-02-22
    标题:Synthesis of novel xylosides and potential uses thereof
    发明人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM
    权利人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM
    摘要:The present invention includes a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, the xyloside having a chemical structure of one of Formula (1), Formula (2), Formula (3), Formula (4), Formula (5), Formula (6), Formula (7), Formula (8), Formula (9), or Formula (10) as shown herein. Also, the present invention includes a method of making a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, wherein the method is performed with “Clickâ€? chemistry. Additionally, the present invention includes a method of administering a xyloside so as to induce synthesis of a glycosaminoglycan in a cell.

    专利号:US-2008125587-A1
    优先权日:2006-05-25
    标 题 :Synthesis of triazole compounds that modulate HSP90 activity
    发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA
    权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA
    摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:

    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-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    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.
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    主要参考文献


    1: Anekonda TS, Quinn JF. Calcium channel blocking as a therapeutic strategy for Alzheimer's disease: the case for isradipine. Biochim Biophys Acta. 2011 Dec;1812(12):1584-90. doi: 10.1016/j.bbadis.2011.08.013. Epub 2011 Sep 8. Review.
    2: Hansson L. How to study the role of hypertension in atherosclerosis. Lessons from MIDAS. Multicentre Isradipine Diuretic Atherosclerosis Study. Blood Press Suppl. 1996;4:16-9. Review. Review. Italian. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. German.

    合成参考文献


    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    参考文献:10.1016/s0952-3278(96)90021-6
    摘要:Oddis CV, Mayer OH, Finkel MS. Inotropic, chronotropic, and radioligand binding characteristics of leukotriene B4 in cardiac myocyte, papillary muscle, and membrane preparations. Prostaglandins Leukot Essent Fatty Acids. 1996 Mar;54(3):223–8. doi: 10.1016/s0952-3278(96)90021-6.
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