CAS: 53885-35-1; 5-(2-Chlorobenzyl)-4,5,6,7-Tetrahydrothieno[3,2-C]Pyridine Hydrochloride

该化合物是一种三烯丙烯类抗板剂,用于抑制小盘聚集,主要用于预防中风和心肌梗死等血栓事件,其机制包括不可逆转地封锁小盘上的P2Y12二氧磷酸酯受体,减少其活化和随后的凝块形成;该化合物对于不耐阿司匹林或需要替代抗塑剂治疗的病人特别宝贵;它显示出行动延迟的开始,经过几天的施药后达到了峰值;三洛匹丁盐盐是代谢性肝化的,需要监测潜在的有害影响,包括中微粒素或血栓球,其临床效用在于其目标抑制板状功能,在抗血清剂中提供独特的药理学特征.

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54903-50-3 4,5,6,7-四氢噻吩并[3... | CAS号108-20-3 异丙醚 | CAS号611-19-8 邻氯氯苄 | CAS号60612-23-9 N-(2-氯苄基)-2-(-2... | CAS号18997-19-8 特戊酸氯甲酯 | CAS号69061-17-2 N-(2-氯苄基)-2-(2-... | CAS号505-23-7 1,3-二噻烷 | CAS号646-06-0 1,3-二氧戊环 | CAS号107-30-2 氯甲基甲醚 | CAS号30433-91-1 2-噻吩乙胺

合成工艺路线路线简述

    N-(2-氯苄基)-2-(-2-噻吩基)乙胺盐酸盐置于盐酸体系中,用 1,3-二噁烷,水 作为反应溶剂,化学反应 6.0H,以82%的收率获得产物盐酸噻氯匹定
    参考文献:制备盐酸噻氯匹定的新方法
    标题:制备盐酸噻氯匹定的新方法
    摘要:本发明提供了一种制备盐酸噻氯匹定的新方法,以噻吩乙醇作为原料,在缚酸剂的作用下,先和对甲苯磺酰氯反应对羟基进行保护活化羟基;再和邻氯苄胺进行缩合反应;然后在酸性条件下,和1,3-二氧五环进行关环反应得盐酸噻氯匹定.其反应条件温和,生产成本低,产品收率高,质量好,便于工业化生产.

    海关参考信息

    专利信息


    专利号:EP-0439404-B1
    优先权日:1990-01-25
    标题 :Preparation of 2-(2'-thienyl) alkylamines and derivatives thereof and synthesis of 4,5,6,7- thieno [3,2-c] pyridine derivatives therefrom
    发明人:KHATRI HIRALAL N; DEHOFF BRADLEY S
    权利人:SANOFI SA
    摘要:An improved process for the synthesis of 2-(2 min -thienyl)ethylamine from suitably functionalized derivatives of 2-(2 min -thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2 min -thienyl)ethylamine produced by this process is advantageously converted to the carbamic acid salt, which is suitably reconverted to 2-(2 min -thienyl)ethylamine, a useful intermediate in the synthesis of ticlopidine.

    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-5068360-A
    优先权日:1990-01-25
    标题 :Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno(3,2-C)pyridine derivatives therefrom
    发明人:DEHOFF BRADLEY S
    权利人:SYNTEX INC
    摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.

    专利号:US-5191090-A
    优先权日:1990-01-25
    标题:Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno[3,2-c]pyridine derivatives therefrom
    发明人:DEHOFF BRADLEY S
    权利人:SYNTEX INC
    摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.

    专利号:US-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:US-4997945-A
    优先权日:1990-01-25
    标 题:Carbamate salts of 2-(2'-thienyl)alkylamines
    发明人:KHATRI HIRALAL N
    权利人:SYNTEX INC
    摘要:The carbamate salt of 2-(2'-thienyl)-alkylamines and particularly the ethylamine and its method of synthesis are disclosed. The carbamate salt of 2-(2'-thienyl)ethylamine is a stable, easily transportable crystalline material that can be converted to 2-(2'-thienyl)ethylamine, a useful intermediate in the synthesis of 5[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine hydrochloride, also known as ticlopidine hydrochloride. The synthesis is carried out by reacting an amine of formula (I): (I) with CO2 in a hydrocarbon solvent to obtain the carbamate salt of formula II: II
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    📌 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: Jacob S, Dunn BL, Qureshi ZP, Bandarenko N, Kwaan HC, Pandey DK, McKoy JM, Barnato SE, Winters JL, Cursio JF, Weiss I, Raife TJ, Carey PM, Sarode R, Kiss JE, Danielson C, Ortel TL, Clark WF, Rock G, Matsumoto M, Fujimura Y, Zheng XL, Chen H, Chen F, Armstrong JM, Raisch DW, Bennett CL. Ticlopidine-, clopidogrel-, and prasugrel-associated thrombotic thrombocytopenic purpura: a 20-year review from the Southern Network on Adverse Reactions (SONAR). Semin Thromb Hemost. 2012 Nov;38(8):845-53. doi: 10.1055/s-0032-1328894. Epub 2012 Oct 30. Review.
    2: Moore TJ, Bennett CL. Underreporting of hemorrhagic and thrombotic complications of pharmaceuticals to the U.S. Food and Drug Administration: empirical findings for warfarin, clopidogrel, ticlopidine, and thalidomide from the Southern Network on Adverse Reactions (SONAR). Semin Thromb Hemost. 2012 Nov;38(8):905-7. doi: 10.1055/s-0032-1328890. Epub 2012 Oct 21. Review.
    3: Kaul U, Mansoor AH. Platelet adenosine diphosphate receptor antagonists: ticlopidine to ticagrelor-a long continuing journey. Indian Heart J. 2012 Jan-Feb;64(1):54-9. doi: 10.1016/S0019-4832(12)60012-1. Epub 2012 Mar 26. Review.

    合成参考文献


    参考文献:10.1007/s00701-011-1084-4
    摘要:Saito A, Shimizu H, Fujimura M, Inoue T, Tominaga T. Predictive role of modified clinical diffusion mismatch in early neurological deterioration due to atherothrombotic ischemia in the anterior circulation. Acta Neurochir (Wien). 2011 Nov;153(11):2205–10. doi: 10.1007/s00701-011-1084-4.
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