CAS: 286930-03-8; (R)-2-(3-(Diisopropylamino)-1-Phenylpropyl)-4-(Hydroxymethyl)Phenyl Isobutyrate Fumarate

该化合物是一种主要用作抗氨酸剂治疗过活性膀胱的药物化合物,是一种代谢为活性形式的5-氢氧甲基异丁二烯,有选择性地抑制膀胱的肌肉受体,从而减少非自愿收缩,增加膀胱的容量.该物质一般是口服的,以其相对有利的副作用而闻名于其他抗胆碱药物.Fesoterodine fumrate的特点是其在水和有机溶剂中的溶性,有利于其在胃肠道中吸收.该化合物的分子结构包括一种丰酸盐,增强它的稳定性和生物利用率.常见副作用可能包括干口,静脉和眩晕,这是抗胆碱药物的典型特征.与任何药物一样,在医疗监督下使用fesoterodine fumate,以确保适当施用并监测潜在不利影响.

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fesoterodine (2E)-but-2-enedioic acid isobutyryl chloride (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)-phenol

合成工艺路线路线简述

    📜(R)-5-羟甲基托特罗定置于三乙胺体系中,用 二氯甲烷,环己烷,丁酮 用作溶剂,化学反应 21.92H,反应生成富马酸非索罗定
    参考文献: Short Synthesis Of Tolterodine,Intermediates And Metabolites[fr] Synthèse Courte De Toltéropine,Intermédiaires Et Métabolites
    标题: Short Synthesis Of Tolterodine,Intermediates And Metabolites[fr] Synthèse Courte De Toltéropine,Intermédiaires Et Métabolites
    摘要:描述了一种用于制备中间体的过程,这些中间体可用于制备尿失禁治疗药物,特别是用于2-(3-(二异丙基氨基)-1-苯基丙基)-4-(羟甲基)苯酚及其前药的制备.

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    专利信息


    专利号:US-7985873-B2
    优先权日:2006-06-09
    标题:Synthesis of phenolic esters of hydroxymethyl phenols
    发明人:ENNIS SETH C; DREWS ROLAND; MEESE CLAUS
    权利人:UCB PHARMA GMBH
    摘要:The present invention provides a process for the production of a compound of formula (I) or a salt thereof, wherein R is hydrogen, a straight, branched or cyclic C 1 -C 6 alkyl group or an aryl group which may optionally be substituted. This process comprises: (a) reacting a compound of formula (II), with a compound of formula (III), wherein R is as defined above and X is a leaving group, in the presence of N,N-di-isopropylethylamine.

    专利号:US-9751828-B2
    优先权日:2014-07-30
    标题:Antimuscarinic compound having a low content of impurities
    发明人:ALLEGRINI PIETRO; ATTOLINO EMANUELE; GRAZIOSI RENZO
    权利人:DIPHARMA FRANCIS SRL
    摘要:Substantially stable to degradation Fesoterodine fumarate, a process for its preparation and a process for the synthesis of specific degradation impurities of Fesoterodine fumarate are disclosed.

    专利号:WO-2014012832-A1
    优先权日:2012-07-16
    标 题:Process for the preparation of 2-(3-n,n-diisopropylamino-1-phenylpropyl)-4-hydroxymethyl-phenol and its derivatives
    发明人:PICCOLO ORESTE; GIANNINI ELIOS; BIGINI LAURA; GIANOLLI EDOARDO; VIGO DANIELE
    权利人:CAMBREX PROFARMACO MILANO S R L
    摘要:The invention concerns a process for the preparation of 2-(3-N,N- diisopropylamino-l-phenylpropyl)-4-hydroxymethyl-phenol and its derivatives, particularly the corresponding (R) 4-trityloxymethyl derivative, useful as intermediate form in the synthesis of Fesoterodine and its salts, in particular for the preparation of Fesoterodine fumarate salt.

    专利号:ES-2350611-T3
    优先权日:2006-06-09
    标 题 :SYNTHESIS OF PHENOLIC ESTERS OF HYDROXYMETHYLPHENOLS.

    专利号:WO-2011110556-A1
    优先权日:2010-03-09
    标 题:Short synthesis of tolterodine, intermediates and metabolites

    专利号:CA-2648333-C
    优先权日:2006-06-09
    标 题:Synthesis of phenolic esters of hydroxymethyl phenols

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    主要参考文献


    1: Gomelsky A, Dmochowski RR. Fesoterodine fumarate. Drugs Today (Barc). 2010 Feb;46(2):81-90. doi: 10.1358/dot.2010.46.2.1437712. 15(3):385-93. doi: 10.1517/14656566.2014.875158. Epub 2013 Dec 27. 2006–. Fesoterodine. 2021 Aug 16. 2012–. Fesoterodine. 2023 Jul 12. 9(12):1659-66. doi: 10.1517/17425255.2013.858118. Epub 2013 Nov 9. 69(6):731-8. doi: 10.2165/00003495-200969060-00006.
    833:155-157. doi: 10.1016/j.ejphar.2018.05.036. Epub 2018 May 24. 38(8):2013-2019. doi: 10.1007/s00345-019-02981-7. Epub 2019 Oct 23. 40(8):2026-2033. doi: 10.1002/nau.24790. Epub 2021 Sep 9. 10(5):805-8. doi: 10.1517/14740338.2011.591377. Epub 2011 Jun 4. 31(6):1201-43. doi: 10.1185/03007995.2015.1032917. Epub 2015 Apr 23. 25(1):72-78. doi: 10.5770/cgj.25.530.
    13: Wyndaele JJ, Schneider T, MacDiarmid S, Scholfield D, Arumi D. Flexible dosing with fesoterodine 4 and 8 mg: a systematic review of data from clinical trials. Int J Clin Pract. 2014 Jul;68(7):830-40. doi: 10.1111/ijcp.12425. Epub 2014 Apr 22. 27(6):e212-e213. doi: 10.1097/RHU.0000000000000932. 71(5):273-88. doi: 10.1016/j.curtheres.2010.10.003.
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