CAS: 74050-98-9; 3-(2-(4-(4-Fluorobenzoyl)Piperidin-1-yl)Ethyl)Quinazoline-2,4(1H,3H)-Dione

该化合物是一种制药化合物,主要因其作为5-HT2A血清素5-HT2A受体的选择性敌国而得到公认,被归类为抗血压剂,并被调查其在治疗各种心血管疾病方面的潜力. Ketanserin 展示了一种独特的行动机制,阻塞血清素受体,这可能导致血管血管血管炎并随后降低血压.该化合物通常以盐的形式施用,以其温和的亲口性闻名,允许其有效跨过生物膜.除了其抗血压特性外,Ketanserin还因其对其他...

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上下游产品

4-(4-fluorobenzoyl)piperidine hydr°Chloride 4-methyl-2-pentanone 3-(2-chloroethyl)-2,4-dioxo-1,2,3,4-tetrahydroquinazoline 2,4-Dioxo-3-(2-hydroxyethyl)-1,2,3,4-tetrahydroquinazoline2-[3-{2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl}-2,4-dioxo-3,4-dihydro-1(2H)-quinazolinyl]-N,N-dimethylacetamide hydr°Chloride Ketanserinol ketanserin tartrate

合成工艺路线路线简述

    邻氨基苯甲酸甲酯置于氯化亚砜,Sodium Carbonate体系中,用 四氢呋喃,5,5-Dimethyl-1,3-Cyclohexadiene,水,1,2-二氯乙烷,甲苯,乙腈 作为反应溶剂,化学反应 73.0H,反应生成 凯他色林
    参考文献:一种酮色林中间体以及酮色林的制备方法
    标题:一种酮色林中间体以及酮色林的制备方法
    摘要:本发明公开了一种酮色林中间体2,3‑二氢‑5H‑噁唑并[2,3‑b]喹唑啉‑5‑酮的制备方法和一种酮色林的制备方法,所述酮色林中间体2,3‑二氢‑5H‑噁唑并[2,3‑b]喹唑啉‑5‑酮的制备方法的反应方程式如下:在该反应中,使用碳酸钠和乙腈并且不添加催化剂,反应后热滤除去无机盐,滤液蒸干回收乙腈得到中间体04即酮色林中间体2,3‑二氢‑5H‑噁唑并[2,3‑b]喹唑啉‑5‑酮.该方法操作简便,成本更低,产物性状更好,更有利于最终产物的合成.

    海关参考信息

    专利信息


    专利号:WO-2012017400-A1
    优先权日:2010-08-03
    标 题 :Synthesis of acyl-pantetheine derivatives and the use thereof in the synthesis of acyl-coenzyme a derivatives
    发明人:VAN DIJK ALBERDINA AIKE; BADENHORST CHRISTOFFEL PETRUS STEPHANUS
    权利人:UNIV NORTHWEST; VAN DIJK ALBERDINA AIKE; BADENHORST CHRISTOFFEL PETRUS STEPHANUS
    摘要:The present invention relates to a novel synthesis method for acyl-pantetheine derivatives. The present invention further relates to the use of said synthesized acyl-pantetheine derivatives as a starting material in the enzymatic synthesis of acyl-coenzyme A derivatives. According to a first aspect thereof, the present invention provides a method for the synthesis of acyl-pantetheine derivatives, the method including the steps of: a) providing a source of pantetheine; b) providing a source of acyl ester; and c) contacting the source of pantetheine with the source of acyl ester to form the corresponding acyl-pantetheine derivative, having the general formula (I), wherein R is an acyl group.The present invention also provides a method for the synthesis of acyl-coenzyme A derivatives as well as the use of a source of pantetheine and a source of acyl ester in the preparation steps of these two methods.

    专利号:US-6376667-B1
    优先权日:1997-11-26
    标 题 :Solid phase synthesis of heterocycles
    发明人:CASTELHANO ARLINDO L; SHAO HUI
    权利人:OSI PHARM INC
    摘要:Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.

    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-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-6469065-B1
    优先权日:1996-02-02
    标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
    发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

    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: Singh S, Dinesh N, Kaur PK, Shamiulla B. Ketanserin, an antidepressant, exerts its antileishmanial action via inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) enzyme of Leishmania donovani. Parasitol Res. 2014 Jun;113(6):2161-8. doi: 10.1007/s00436-014-3868-y. Epub 2014 Apr 12. doi: 10.1016/j.ejogrb.2015.02.002. Epub 2015 Mar 10. doi: 10.1002/lt.23947. doi: 10.1016/j.ejphar.2013.09.043. Epub 2013 Sep 25. doi: 10.1016/j.pbb.2013.10.024. Epub 2013 Nov 4.
    6: Aljuffali IA, Brainard BM, Moore JN, Kwon S, Allen D, Robertson TP, Arnold RD. Pharmacokinetic assessment of ketanserin in the horse. J Vet Pharmacol Ther. 2012 Oct;35(5):472-7. doi: 10.1111/j.1365-2885.2011.01346.x. Epub 2011 Nov 18. doi: 10.1016/j.ejogrb.2012.01.013. Epub 2012 Feb 19. doi: 10.1093/infdis/jir609. Epub 2011 Sep 14. doi: 10.1016/j.phrs.2011.02.009. Epub 2011 Mar 21. doi: 10.1016/j.bbr.2011.04.045. Epub 2011 May 7.
    12: Coha B, Samardžić P, Dundjer I, Knežević-Praveček M. Cardiac arrhythmia as a side effect of ketanserin therapy in a patient with systemic scleroderma. Acta Dermatovenerol Croat. 2012;20(1):54-6. doi: 10.1016/j.ejphar.2009.11.011. Epub 2009 Nov 11. doi: 10.1016/j.euroneuro.2012.10.006. Epub 2012 Nov 21.

    合成参考文献


    参考文献:10.1186/2047-783x-14-s4-32
    摘要:Budzinska K. Serotoninergic modulation of cortical and respiratory responses to episodic hypoxia. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):32. doi: 10.1186/2047-783x-14-s4-32.
    参考文献:10.3389/fnbeh.2011.00031
    摘要:Xu H, Yang HJ, Rose GM, Li XM. Recovery of behavioral changes and compromised white matter in C57BL/6 mice exposed to cuprizone: effects of antipsychotic drugs. Front Behav Neurosci. 2011;5():31.
    参考文献:10.1242/jeb.056333
    摘要:Regan KS, Jonz MG, Wright PA. Neuroepithelial cells and the hypoxia emersion response in the amphibious fish Kryptolebias marmoratus. J Exp Biol. 2011 Aug 01;214(Pt 15):2560–8. doi: 10.1242/jeb.056333.
    参考文献:10.1177/0269881111408958
    摘要:Ruehle S, Rey AA, Remmers F, Lutz B. The endocannabinoid system in anxiety, fear memory and habituation. J Psychopharmacol. 2012 Jan;26(1):23–39.
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