CAS: 64169-39-7; 5-Bromodescyano Citalopram

该化合物是高血清的衍生物,一种选择性的血清素再摄取抑制剂(SSRI),该化合物在phthalane环的5个位置上具有溴替代物,没有母分子中含有的西诺组,结构改变可能会影响其药用动力学和药用动力学特性,有可能改变与血清素运输器(SERT)的结合性.它作为药物化学研究的宝贵中间体,用于探索SMI类生物的结构活动关系(SAR).溴混合物会增强其在进一步合成转化中的效用,例如交叉反应,使其成为开发新型...

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    CAS号488148-10-3 1-[4-BROMO-2-(H... | CAS号508169-73-1 1-[4-溴-2-(羟基甲基)... | CAS号59729-33-8 西酞普兰 | CAS号62498-67-3 Desmethylcitalopram

    合成工艺路线路线简述

      📜1-[4-溴-2-(羟基甲基)苯基]-4-(二甲基氨基)-1-(4-氟苯基)-1-丁醇盐酸盐置于磷酸,氨体系中,用 水,甲苯 作为反应溶剂,化学反应 2.5H,以93.6%的收率获得产物3-(5-溴-1-(4-氟苯基)-1,3-二氢异苯并呋喃-1-基)-N,N-二甲基丙烷-1-胺
      参考文献:シタロプラムの製造方法
      标题:シタロプラムの製造方法
      摘要:本发明提供了一种生产已知抗抑郁药西酞普兰的新方法.

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      专利信息


      专利号:US-2008119662-A1
      优先权日:2004-02-16
      标 题:One Spot Synthesis of Citalopram from 5-Cyanophthalide
      发明人：NARAHARI BABU AMBATI; SRINIVAS GOUD VUDDAMARI; GAONKAR SANTOSH LAXMAN; MANJUNATHA SULUR G; KULKARNI ASHOK KRISHNA; KULKARNI MADHARI A
      权利人:JUBILANT ORGANOSYS LIMTED
      摘要:A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5-cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.

      专利号:CA-2559703-A1
      优先权日:2004-02-16
      标 题:One pot synthesis of citalopram from 5-cyanophthalide

      专利号:WO-2005077927-A1
      优先权日:2004-02-16
      标 题:One pot synthesis of citalopram from 5-cyanophthalide

      专利号:EP-1723133-A1
      优先权日:2004-02-16
      标 题:One pot synthesis of citalopram from 5-cyanophthalide

      专利号:IT-MI991486-A1
      优先权日:1999-07-06
      标 题:PROCESS FOR THE SYNTHESIS OF CITALOPRAM

      专利号:WO-0102383-A2
      优先权日:1999-07-06
      标题 :Process for the synthesis of citalopram

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      主要参考文献

      参考标题:Ex Situ Generation Of Stoichiometric Hcn And Its Application In The Pd-Catalysed Cyanation Of Aryl Bromides: Evidence For A Transmetallation Step Between Two Oxidative Addition Pd-Complexes
      作者:Steffan K. Kristensen,Espen Z. Eikeland,Esben Taarning,Anders T. Lindhardt,Troels Skrydstrup
      摘要:Methodology Was Also Suitable For The Synthesis Of 13C-Labelled Benzonitriles With Ex Situ Generated 13C-Hydrogen Cyanide. Stoichiometric Studies With The Metal Complexes Were Undertaken To Delineate The Mechanism For This Catalytic Transformation. Treatment Of Pd(P(Tbu)3)2 With H13Cn In Thf Provided Two Pd-Hydride Complexes, (P(Tbu)3)2Pd(H)(13Cn), And [(P(Tbu)3)Pd(H)]2Pd(13Cn)4, Both Of Which Were Isolated

      合成参考文献


      摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 361.
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