CAS: 147-20-6; 4-(Benzhydryloxy)-1-Methylpiperidine

该化合物是乙醇胺类的一种抗脊髓灰质炎化合物,主要用于对H1甲胺受体产生对抗效应,通过竞争抑制丁胺结合,在减轻过敏反应方面表现出显著的功效,从而通过抑制苯丙胺结合,从而减少了普里图斯,尿道和犀牛等症状.其分子结构增强了亲脂性,促进了高效的血液阻塞渗透,从而助长了其镇静特性.二苯丙胺与其他活性成分一起配制,常常在多症状的抗药性制剂中增加治疗结果.该化合物在标准储存条件下表现出稳定性,确保可靠的储存寿命.其特性良好的药理基因特征支持了可预测的吸收和代谢,从而在临床应用中成为了一种连贯的选择.

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合成工艺路线路线简述

    📜4-羟基哌啶置于potassium Carbonate,对甲苯磺酸体系中,用 N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应生成双苯拉林
    参考文献:新型n-取代的4-(芳甲氧基)哌啶作为多巴胺转运蛋白抑制剂的合成与生物学评价
    标题:新型n-取代的4-(芳甲氧基)哌啶作为多巴胺转运蛋白抑制剂的合成与生物学评价
    摘要:设计并合成了新的n-取代的4-(芳基甲氧基)哌啶作为多巴胺转运蛋白抑制剂的库.发现哌啶环中的h键供体对于降低小鼠的运动活性很重要.4-[双(4-氟苯基)甲氧基]哌啶对多巴胺转运蛋白和运动活性的ic50为17.0+/-1.0 Nm,低于可卡因的ic50.
    Doi:10.1016/j.Mencom.2019.03.030

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    专利信息


    专利号:WO-2025136243-A1
    优先权日:2023-12-20
    标题:Mechanochemical synthesis of histamine h1-receptor antagonists
    发明人：AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA
    权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT
    摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.

    专利号:US-2013030282-A1
    优先权日:2011-07-18
    标题:Synthesis and characterization of near ir fluorescent magnetic and non-magnetic albumin nanoparticles for biomedical applications
    发明人：MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL
    权利人:UNIV BAR ILAN; MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL
    摘要:The present invention discloses Near Infrared (NIR) fluorescent albumin nanoparticles having a structure selected from a core structure or a core-shell structure. Also disclosed are a process of preparing these NIR fluorescent albumin nanoparticles, and a method of in vivo detection of pathologies, in particular cancer pathology, by using administering these NIR fluorescent albumin nanoparticles to a patient.

    专利号:CN-1740157-A
    优先权日:2005-09-02
    标 题:Synthesis process of N-sustituent-4-piperidyl alcohol

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    主要参考文献


    1: Oleson EB, Ferris MJ, España RA, Harp J, Jones SR. Effects of the histamine H₁ receptor antagonist and benztropine analog diphenylpyraline on dopamine uptake, locomotion and reward. Eur J Pharmacol. 2012 May 15;683(1-3):161-5. doi: 10.1016/j.ejphar.2012.03.003. Epub 2012 Mar 15.
    2: Montijo-Barrios E, Cadena F, Ramírez-Mayans JA, Gutiérrez-Castrellón P. [Clinical trial on the effect of buphenine, aminophenazone and diphenylpyraline hydrochloride in treating the common cold in children of 6 to 24 months of age]. Rev Invest Clin. 2011 Jul-Aug;63(4):335-43. Spanish. Epub 2007 Jul 10. Epub 2007 Jun 16. Epub 2004 Dec 8. German. Swedish. German. Spanish.

    合成参考文献


    摘要:Therapie., 26(1203), 1971 []
    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    摘要:COMOES S, MORAES JB, CAZZALINO JD. [Clinical study of diphenylpyraline]. Hospital (Rio J). 1958 Sep;54(3):317–21.
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