CAS: 14008-44-7; 1-[3-(2-Methylsulfonylphenothiazin-10-yl)Propyl]Piperidine-4-Carboxamide

该化合物是一种具有强效抗乳性特性的苯并硫胺衍生物,主要作为多巴胺D2受体对立剂,临床上用于对恶心和呕吐进行管理,特别是在胃肠炎和手术后环境下,它有选择地与 medulla obloongata 中的乳腺受体触发区(CTZ)有约束力,确保有效抑制乳胶,降低与老的苯并胺相比的过量效应风险.Metopimazine对其他受体系统表现出低亲近性,有助于其有利于可耐性特征.在口服和注射的配方中,它为急性和预防性抗乳酸疗法提供了灵活的服药选择.它的药用能支持可预见效果,但只有最小的节能.

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欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

2-(2-fluorophenylthio)-5-(methylsulfonyl)aniline 2-(2-fluorophenylthio)-5-(methylsulfonyl)nitrobenzene 4-carboxamidopiperidine 10-(3-chloropropyl)-2-(methylsulfonyl)-10H-phenothiazinemetopimazine acid

合成工艺路线路线简述

    📜2-硝基-4-甲砜基氯苯置于盐酸,Hydrazine Hydrate,Iron(III) Chloride Hexahydrate,三乙酰氧基硼氢化钠,Sodium Hydride,Potassium Carbonate,甲烷,溶剂黄146,Potassium Hydroxide体系中,用 乙醇,二氯甲烷,水,二甲基亚砜,丙酮 用作溶剂,化学反应 24.0H,反应生成美托哌丙嗪
    参考文献:一种制备美托哌丙嗪的新工艺
    标题:一种制备美托哌丙嗪的新工艺
    摘要:本发明揭示了一种制备美托哌丙嗪的新工艺,在反应器中,以邻氟苯硫酚和邻硝基对甲砜基氯苯为原料,在丙酮中反应得2‑(2‑氟苯基硫基)‑5‑(甲基磺酰基)硝基苯;然后加乙醇,三氯化铁加热反应,生成2‑(2‑氟苯基硫基)‑5‑(甲基磺酰基)苯胺;再加入二甲基亚砜,加入nah,升温反应,降至室温后加入水搅拌,制得2‑甲磺酰基‑10H‑吩噻嗪;随后加10‑乙酰基‑2‑甲亚砜基‑10H吩噻嗪,氢氧化钾反应制得10‑乙酰基‑2‑甲磺酰基‑(5‑亚砜基)‑10H吩噻嗪;再加入丙酮,通过浓缩萃取,得到10‑乙酰基‑2‑甲磺酰基‑10H吩噻嗪的二氯甲烷溶液,降温后加哌啶‑4‑甲酰胺,加醋酸硼氢化钠,反应过滤,滤饼打浆得美托哌丙嗪;本发明通过优化反应路线和反应条件,使得最终收率得到了很大的提高,产品纯度高达99.3%以上.

    海关参考信息

    专利信息


    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:WO-0054773-A1
    优先权日:1999-03-12
    标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC; GARVEY DAVID S
    摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

    专利号:EP-3103803-B1
    优先权日:2008-10-27
    标 题 :Intermediates for the synthesis of mtor kinase inhibitors

    专利号:CA-2555219-A1
    优先权日:2004-02-03
    标 题 :Synthesis of cyanoimino-benzoimidazoles

    专利号:US-11759496-B2
    优先权日:2016-05-10
    标题:Compounds and pharmaceutical use thereof in the treatment of cancer
    发明人:SUSIN SANTOS A; KAROYAN PHILIPPE; MERLE-BERAL HÉLÈNE
    权利人:KAROYAN PHILIPPE
    摘要:The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.

    专利号:WO-2005075459-A1
    优先权日:2004-02-03
    标题:Synthesis of cyanoimino-benzoimidazoles

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Rochoy M, Auffret M, Béné J, Gautier S; Réseau français des centres régionaux de pharmacovigilance. [Antiemetics and cardiac effects potentially linked to prolongation of the QT interval: Case/non-case analysis in the national pharmacovigilance database]. Rev Epidemiol Sante Publique. 2017 Feb;65(1):1-8. doi: 10.1016/j.respe.2016.06.335. Epub 2016 Dec 14. French. doi: 10.1002/prp2.130. Epub 2015 Jun 1.
    3: Roussel V, Tritz T, Souty C, Turbelin C, Arena C, Lambert B, Lillo-Lelouët A, Kernéis S, Blanchon T, Hanslik T. Estimating the excess of inappropriate prescriptions of anti-dopaminergic anti-emetics during acute gastroenteritis epidemics in France. Pharmacoepidemiol Drug Saf. 2013 Oct;22(10):1080-5. doi: 10.1002/pds.3486. Epub 2013 Aug 12. doi: 10.1002/jms.1790. doi: 10.1016/j.ejmech.2010.05.021. Epub 2010 May 15. doi: 10.1577/H08-030.1. doi: 10.2165/11316190-000000000-00000. Review. doi: 10.1097/SPC.0b013e3282f44a75. Review. doi: 10.1016/j.jdermsci.2008.06.009. Epub 2008 Aug 3. doi: 10.1080/03639040701743873 . doi: 10.1016/j.patbio.2007.09.003. Epub 2008 Jan 4. French. Epub 2006 Dec 19. Epub 2006 Dec 11. Epub 2006 Nov 9. Erratum in: Anticancer Drugs. 2006 Jun;17(5):599. Khamales, Slimane [added]. Epub 2005 Jul 29. Review.

    合成参考文献


    摘要:Comptes Rendus des Seances de l'Academie des Sciences, Serie D: Sciences Naturelles., 266(2365), 1968
    摘要:Psychotropic Drugs and Related Compounds, 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972, -(32), 1972
    参考文献:10.2165/00002512-199609030-00003
    摘要:Montastruc JL, Rascol O, Senard JM. New directions in the drug treatment of Parkinson's disease. Drugs Aging. 1996 Sep;9(3):169–84. doi: 10.2165/00002512-199609030-00003.
    参考文献:10.1038/sj.bjc.6690372
    摘要:Sigsgaard T, Herrstedt J, Andersen LJ, Havsteen H, Langer SW, Kjærbøl A, Lund H, Kjær M, Dombernowsky P. Granisetron compared with prednisolone plus metopimazine as anti-emetic prophylaxis during multiple cycles of moderately emetogenic chemotherapy. British Journal of Cancer. 1999 Apr 09;80(3-4):412–8. doi: 10.1038/sj.bjc.6690372.
    参考文献:10.2165/00002018-199309060-00004
    摘要:Del Favero A, Roila F, Tonato M. Reducing chemotherapy-induced nausea and vomiting. Current perspectives and future possibilities. Drug Saf. 1993 Dec;9(6):410–28. doi: 10.2165/00002018-199309060-00004.
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