CAS: 19237-84-4; (4-(4-Amino-6,7-Dimethoxyquinazolin-2-yl)Piperazin-1-yl)(Furan-2-yl)Methanone Hydrochloride

该化合物是一种主要用作抗血压剂和治疗良性先天性增生症症状的药物化合物,属于甲型-1肾上腺对抗者一类药物,该类药物在血管中阻塞甲型-1受体,导致血管血管变异和减少血压.该物质似乎是白色的脱白晶粉,溶于水和酒精,有利于以多种剂量形式配制该物质.盐酸丙胺一般是口服的,其半衰期相对较短,需要全天多剂量才能产生持续治疗效果.常见副作用可能包括眩晕,头痛和或敌意性偏执,特别是在开始治疗时.其行动机制还有助于通过减轻恶梦治疗创伤后应激障碍(PCDD)等症状.与任何药物一样,必须在医疗监督下使用盐酸丙胺来监测潜在的相互作用和副作用.

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CAS号67817-59-8 Methyl N-(3,4-D... | CAS号527-69-5 糠酰氯 | CAS号123-51-3 异戊醇 | CAS号60547-97-9 2-(1-哌嗪基)-4-氨基-... | CAS号26961-27-3 2-氨基-4,5-二甲氧基苯腈 | CAS号43091-89-0 3,4-Dimethoxy-6... | CAS号67817-56-5 N-(2-cyano-4,5-... | CAS号63590-64-7 特拉唑嗪

合成工艺路线路线简述

    Methyl N-(3,4-Dimethoxy-6-Cyanophenyl)-<4-(2-Furoyl)Piperazin-1-Yl>Thioformamidate置于ammonium Chloride体系中,用 Formamide 用作溶剂,化学反应 20.0H,以86%的收率获得盐酸哌唑嗪
    参考文献:哌唑嗪的新实用合成
    标题:哌唑嗪的新实用合成
    摘要:已经描述了新的四步合成哌唑嗪2-[4-(2-呋喃基)哌嗪-1-基]-4-氨基-6,7-二甲氧基喹唑啉.该方法也适用于制备其他取代的4-氨基喹唑啉.在每个步骤中产率都很高,并且反应容易进行.在最后一步中直接获得了高纯度的哌唑嗪盐酸盐.
    Doi:10.1002/jhet.5570170436

    海关参考信息

    专利信息


    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-6387893-B1
    优先权日:1999-09-30
    标题 :Spirotricyclic substituted azacycloalkane derivatives and uses thereof
    发明人:EVANS BEN E; HOFFMAN JACOB M; GILBERT KEVIN F; RITTLE KENNETH E
    权利人:MERCK & CO INC
    摘要:Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

    专利号:US-6130218-A
    优先权日:1996-12-20
    标 题 :Polymorphic form of doxazosin mesylate (Form I)
    发明人:MOERSDORF JOHANN PETER; GRAFE INGOMAR
    权利人:HEUMANN PHARMA GMBH & CO
    摘要:A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 15.40°, 16.85°, 18.06°, 24.15° and 25.81°. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.

    专利号:US-6133269-A
    优先权日:1996-12-20
    标题:Polymorphic form of doxazosin mesylate (form II)
    发明人:MOERSDORF JOHANN PETER; GRAFE INGOMAR
    权利人:HEUMANN PHARMA GMBH & CO
    摘要:A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 10.68°, 14.45°, 17.37°, 23.45°, 23.82° and 24.30 °. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.

    专利号:US-6232318-B1
    优先权日:1998-11-12
    标 题:Pyrimidinedione derivatives useful as alpha 1A adrenoceptor antagonists
    发明人:NERENBERG JENNIE B; BOCK MARK G
    权利人:MERCK & CO LTD
    摘要:Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

    专利号:US-6326372-B1
    优先权日:1999-09-30
    标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists
    发明人:EVANS BEN E; GILBERT KEVIN F
    权利人:MERCK & CO INC
    摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
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    主要参考文献


    1: Ansari E, Honarvar B, Sajadian SA, Arab Aboosadi Z, Azizi M. Utilization of RESOLV with polymer to produce prazosin hydrochloride nanoparticles and optimization of the process parameters. Sci Rep. 2024 Aug 7;14(1):18346. doi: 10.1038/s41598-024-69128-6.
    2: Sudaki H, Fujimoto K, Wada K, Sugano K. Phosphate buffer interferes dissolution of prazosin hydrochloride in compendial dissolution testing. Drug Metab Pharmacokinet. 2023 Aug;51:100519. doi: 10.1016/j.dmpk.2023.100519. Epub 2023 Jun 10. 11(47):29441-29452. doi: 10.1039/d1ra04758b.
    4: Mazeh AC, Angus JA, Wright CE. Pharmacological characterisation of the CB1 receptor antagonist activity of cannabidiol in the rat vas deferens bioassay. Eur J Pharmacol. 2021 Oct 15;909:174433. doi: 10.1016/j.ejphar.2021.174433. Epub 2021 Aug 17.

    合成参考文献


    摘要:Human Toxicology., 4(53), 1985 []
    摘要:JAMA, Journal of the American Medical Association., 238(157), 1977 []
    摘要:New Cardiovascular Drugs., 4(1), 1986
    摘要:U.S. Department of Health, Education & Welfare, Public Health Service. Center for Disease Control, National Institute for Occupational Safety & Health. Registry of Toxic Effects of Chemical Substances. 1978 edition. Washington, DC: U.S. Government Printing Office, 1979., p. 1108
    摘要:McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2002. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2002 (Plus Supplements)., p. 1862
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