CAS: 26864-56-2; 4-Piperidinol,1-[4,4-Bis(4-Fluorophenyl)Butyl]-4-[4-Chloro-3-(Trifluoromethyl)Phenyl]-

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CAS号21928-50-7 4-[4-氯-3-(三氟甲基)... | CAS号57668-61-8 1,1'-(4-bromobu... | CAS号345-92-6 4,4'-二氟二苯甲酮 | CAS号357-77-7 1,1-二(4-氟苯基)-2-1-丙醇 | CAS号293729-65-4 5,5-bis(4-fluor... | CAS号337506-83-9 1,1-bis(4-fluor... | CAS号50337-85-4 4,4-bis(4-fluor...

合成工艺路线路线简述

    5,5-Bis(4-Fluorophenyl)Oxolan-2-Ol置于10% Palladium On Active Carbon Sodium Hydroxide,Sodium Tetrahydroborate,氢气,溴,Sodium Carbonate,三苯基膦,Potassium Iodide体系中,用 甲醇,乙醇,甲苯,乙腈 用作溶剂,化学反应 5.0H,反应生成五氟利多
    参考文献:铑催化1,1-双(对氟苯基)烯丙基或炔丙醇的加氢甲酰化:氟吡咯啉和戊氟哌啶醇合成的关键步骤
    标题:铑催化1,1-双(对氟苯基)烯丙基或炔丙醇的加氢甲酰化:氟吡咯啉和戊氟哌啶醇合成的关键步骤
    摘要:两种精神抑制药fluspirilen(1)和penfluridol(2)属于一类广泛的药物,其分子中含有与吡咯烷,哌啶或吡咯烷的氮原子结合的4,4-双(对氟苯基)丁基哌嗪部分.按照涉及铑的制备路线,由市售的4,4'-二氟二苯甲酮(7)开始制备用于合成化合物1和2的关键中间体4,4-双(对氟苯基)丁基溴(15).甲苯或双相体系中的催化加氢甲酰化反应甲苯/水或环己烷/ 1,1-双(水)对氟苯基)-2-丙烯醇(8)和/或1,1-双(对氟苯基)-2-丙炔醇(12).Fluspirilen和五氟利均在70-80%的收率获得由溴化反应15与1-苯基-1,3,8-三氮杂螺[4,5]癸烷-4-酮(16)和4-[4-氯-3--(三氟甲基)苯基]-4-哌啶醇(17).基于起始酮7,两种药物1和2的总产率约为35-40%.
    Doi:10.1016/s0040-4020(00)01151-0

    海关参考信息

    专利信息


    专利号:US-2023271983-A1
    优先权日:2020-07-29
    标题 :Functionalized isonitriles and products, preparation and uses thereof
    发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
    权利人:UNIV SANTIAGO COMPOSTELA
    摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

    专利号:MX-2009002267-A
    优先权日:2006-08-28
    标题:PROCEDURE AND INTERMEDIARIES FOR THE SYNTHESIS OF DERIVATIVES AND INTERMEDIARIES OF (3-ALQUIL-5-PIPERIDIN-1-IL-3,3A-DIHIDRO-PIRAZOLO [1,5-A] PIRIMIDIN-7-IL) -AMINO.

    专利号:WO-2025118034-A1
    优先权日:2023-12-06
    标题 :Compounds active at the serotonergic 5-ht2a receptor
    发明人:JORGENSON WILLIAM; TAN JINLONG; WHISH LACHLAN; BANISTER SAMUEL
    权利人:Psylo Pty Ltd
    摘要:The present disclosure relates to compounds of formula (I), their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

    专利号:WO-2023230649-A1
    优先权日:2022-05-30
    标题:Compounds
    发明人:BANISTER SAMUEL; JORGENSEN WILLIAM; TAN JINLONG; WHISH LACHLAN
    权利人:Psylo Pty Ltd
    摘要:The present disclosure relates to compounds of formula (I), their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

    专利号:US-12415804-B2
    优先权日:2023-06-28
    标题 :Compounds for activating a serotonin receptor
    发明人:BANISTER SAMUEL; JORGENSEN WILLIAM; TAN JINLONG; WHISH LACHLAN
    权利人:Psylo Pty Ltd
    摘要:The present disclosure relates generally to compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.
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    主要参考文献


    1: Ranjan A, Gupta P, Srivastava SK. Penfluridol: An Antipsychotic Agent Suppresses Metastatic Tumor Growth in Triple-Negative Breast Cancer by Inhibiting Integrin Signaling Axis. Cancer Res. 2016 Feb 15;76(4):877-90. doi: 10.1158/0008-5472.CAN-15-1233. Epub 2015 Dec 1.
    2: Wu L, Liu YY, Li ZX, Zhao Q, Wang X, Yu Y, Wang YY, Wang YQ, Luo F. Anti-tumor effects of penfluridol through dysregulation of cholesterol homeostasis. Asian Pac J Cancer Prev. 2014;15(1):489-94. doi: 10.1038/srep26165.
    4: Chien W, Sun QY, Lee KL, Ding LW, Wuensche P, Torres-Fernandez LA, Tan SZ, Tokatly I, Zaiden N, Poellinger L, Mori S, Yang H, Tyner JW, Koeffler HP. Activation of protein phosphatase 2A tumor suppressor as potential treatment of pancreatic cancer. Mol Oncol. 2015 Apr;9(4):889-905. doi: 10.1016/j.molonc.2015.01.002. Epub 2015 Jan 15.

    合成参考文献


    参考文献:10.1017/s0031182011000850
    摘要:TRIPATHI R, PANDEY SK, RIZVI A. Clarithromycin, a cytochrome P450 inhibitor, can reverse mefloquine resistance in Plasmodium yoelii nigeriensis- infected Swiss mice. Parasitology. 2011 Jul 15;138(9):1069–76. doi: 10.1017/s0031182011000850.
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