CAS: 15686-51-8; (R)-2-(2-((R)-1-(4-Chlorophenyl)-1-Phenylethoxy)Ethyl)-1-Methylpyrrolidine

该化合物其该化合物其结构复杂,包括一个管状环.其行动机制涉及H1甲胺受体的对抗,从而抑制过敏反应中关键调节者H1胺的影响.除了其抗口炎特性外,颈炎还可能具有抗胆碱效应,这可能会助长其镇静剂的特性.该物质通常通过口服口服,并存在于各种配方中,包括药片和糖浆.由于镇静剂的影响,在使用麻风素后操作机械或驾驶时要小心谨慎.与任何药物一样,潜在的副作用可能包括眩晕,干口和头麻.

结构式图片

上下游产品

(R)-2-[2-[1-(4-Chlorophenyl)-1-Phenylethoxy]Ethyl]-1-Methylpyrrolidine 1174565-35-5
(R)-1-(4-Chlorophenyl)-1-Phenylethanol 117605-76-2

合成工艺路线路线简述

    📜(R)-2-(2-Chloroethyl)-1-Methylpyrrolidine Hydrochloride置于sodium Hydride,Potassium Hydroxide体系中,用 5,5-Dimethyl-1,3-Cyclohexadiene,水,Mineral Oil 用作溶剂,化学反应 4.17H,反应生成富马酸氯马斯汀
    参考文献:H1受体拮抗剂(R,R)-Clemastine的不对称合成
    标题:H1受体拮抗剂(R,R)-Clemastine的不对称合成
    摘要:(R,R)-Clemastine (1) 的第一个不对称合成是通过 (R)-叔醇 2 和 (R)-氯乙基吡咯烷 3 通过 O-烷基化的偶联完成的.(R)-叔醇 2 是通过手性 α-苄氧基酮与格氏试剂通过螯合控制的 1,4-不对称诱导立体选择性烷基化合成的.在反应中,手性苄基作为手性助剂和保护基团.(R)-氯乙基吡咯烷 3 是通过从 L-高丝氨酸内酯开始的不对称转化制备的,其中外消旋化最小化 N-烯丙基化和闭环复分解作为关键步骤.
    Doi:10.1007/s12272-015-0641-4

    海关参考信息

    专利信息


    专利号:US-7919505-B2
    优先权日:2006-07-11
    标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
    发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
    权利人:SCHERING CORP
    摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2011003780-A1
    优先权日:2007-07-10
    标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
    发明人:ZHU MAN
    权利人:SCHERING CORP
    摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

    专利号:US-7402670-B2
    优先权日:2004-09-30
    标 题:Synthesis by chiral diamine-mediated asymmetric alkylation
    发明人:DENG XIAOHU; MANI NEELAKANDHA
    权利人:JANSSEN PHARMACEUTICA NV
    摘要:Chiral synthesis from an achiral starting material by chiral diamine-mediated, such as sparteine-mediated, intermolecular asymmetric alkylation with a strained cyclic ether in the presence of a Lewis acid.

    专利号:WO-2023075715-A1
    优先权日:2021-10-26
    标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids)
    发明人:OYTUN FARUK; CAN EFE
    权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI
    摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.

    专利号:US-11918657-B2
    优先权日:2017-11-10
    标 题 :Dendrimer delivery system and methods of use thereof
    发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH
    权利人:UNIV JOHNS HOPKINS
    摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.

    供应商参考报价(招募中)

    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: Turski CA, Turski GN, Chen B, Wang H, Heidari M, Li L, Noguchi KK, Westmark C, Duncan I, Ikonomidou C. Clemastine effects in rat models of a myelination disorder. Pediatr Res. 2018 May 2. doi: 10.1038/pr.2018.45. [Epub ahead of print] doi: 10.5114/ada.2017.71112. Epub 2017 Oct 31.
    3: Magno Pereira V, Andrade C, Figueira R, Faria G, Jasmins L. Infliximab-Induced Lupus: A Case Report. GE Port J Gastroenterol. 2017 Mar;24(2):84-88. doi: 10.1159/000450877. Epub 2016 Nov 19.
    4: Cree BAC, Niu J, Hoi KK, Zhao C, Caganap SD, Henry RG, Dao DQ, Zollinger DR, Mei F, Shen YA, Franklin RJM, Ullian EM, Xiao L, Chan JR, Fancy SPJ. Clemastine rescues myelination defects and promotes functional recovery in hypoxic brain injury. Brain. 2018 Jan 1;141(1):85-98. doi: 10.1093/brain/awx312. doi: 10.1016/S0140-6736(17)32346-2. Epub 2017 Oct 10. doi: 10.1016/S0140-6736(17)32639-9. Epub 2017 Oct 10. doi: 10.1007/s13311-017-0577-0. Review.

    合成参考文献


    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    参考文献:10.1016/s0379-0738(01)00460-1
    摘要:Gergov M, Robson JN, Ojanperä I, Heinonen OP, Vuori E. Simultaneous screening and quantitation of 18 antihistamine drugs in blood by liquid chromatography ionspray tandem mass spectrometry. Forensic Sci Int. 2001 Sep 15;121(1-2):108–15. doi: 10.1016/s0379-0738(01)00460-1.
    参考文献:10.1007/s002280050144
    摘要:Vuurman EFPM, Muntjewerff ND, Uiterwijk MMC, van Veggel LMA, Crevoisier C, Haglund L, Kinzig M, O'Hanlon JF. Effects of mefloquine alone and with alcohol on psychomotor and driving performance. European Journal of Clinical Pharmacology. 1996 Jul 30;50(6):475–82. doi: 10.1007/s002280050144.
    参考文献:10.1007/bf00203779|10.1007/s002280050033
    摘要:Herrig I, Hoffmann U, Fischer M, Franzeck UK, Bollinger A. Microinjection technique for pharmacological evaluation of microvascular permeability in human skin. European Journal of Clinical Pharmacology. 1996 Feb 01;49(5):365–9. doi: 10.1007/s002280050033.
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