CAS: 124937-53-7; S-(-)-Tolterodine

该化合物是主要用作治疗过活性膀胱的抗肌肉剂的药物化合物,有选择性地抑制膀胱的肌肉受体,从而减少非自愿收缩和增加膀胱容量.该化合物的特征是其性能,其阳性特征是S-enanteomer(相对于R)而言具有更大的威力.S-(-)-Tolterodine(Tolterodine)通常以其酸盐的形式施用,这提高了其溶液和生物利用率.该物质以相对较低的副作用而著称,尽管其常有的不良作用可能包括口干燥,静态和眩晕.其致癌作用主要在于通过细胞色素P450酶,形成各种代谢物.该化合物的化学结构包括一种苯基环和管状胺,有助于其药用活动.

结构式图片

MSDS等安全信息

    上下游产品

    (R)-3-(2-Benzyloxy-5-methyl-phenyl)-N,N-diisopropyl-3-phenyl-propionamide (R)-3-[2-(benzyloxy)-5-methylphenyl]-N,N-diisopropyl-3-phenylpropan-1-amine (4R)-6-methyl-4-phenylchroman-2-ol diisopropylamine2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenylacetate hydr°Chloride 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenylbutyrate hydr°Chloride 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenyl 2-methylpropanoate {4-(benzyloxy)-3-[(1R)-3-(dipropan-2-ylamino)-1-phenylpropyl]phenyl}methanol

    合成工艺路线路线简述

      📜(4S)-6-甲基-4-苯基色满-2-酮置于palladium On Activated Charcoal 氢气,二异丁基氢化铝体系中,用 甲醇,甲苯 用作溶剂,-25.0~48.0 °C,506.66 Kpa 条件下,反应 17.0H,反应生成(S)-托特罗定
      参考文献:通过heck反应获得的香豆素衍生物的不对称加氢,对映体选择性合成(S)-和(R)-托特罗定
      标题:通过heck反应获得的香豆素衍生物的不对称加氢,对映体选择性合成(S)-和(R)-托特罗定
      摘要:(S)-和(R)-托特罗定的有效且短的对映选择性合成是通过香豆素中间体的不对称氢化而进行的,该香豆素中间体容易通过heck反应从廉价且可商购的起始原料中获得.
      Doi:10.1021/jo0705667

      海关参考信息

      专利信息


      专利号:US-10865163-B2
      优先权日:2017-12-20
      标题:Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds
      发明人:YOUNG MICHAEL C; KAPOOR MOHIT
      权利人:UNIV TOLEDO
      摘要:Methods of synthesizing compounds using CO 2 as a directing group for C—H functionalization, and compounds made thereby, are described.

      专利号:US-2007010691-A1
      优先权日:2003-07-02
      标 题:Enantioselective synthesis of enantiomerically enriched compounds
      发明人:PICCOLO ORESS; ULGHERI FAUSTA; MARCHETTI MAURO
      权利人:CONSIGLIO NAZIONALE RICERCHE
      摘要:Method of preparing an enantiomerically enriched compound of formula (II) comprising enantioselective hydrogenation of a compound of general formula (I): where W, X and Z have the meanings indicated in the description, to give a compound of general formula (II): where W, Y, T and C* have the meanings indicated in the description, in the presence of a catalyst or its suitable precursor based on Rh, Ru or Ir, having an oxidation state of 0, +1 or +2, and containing at least one enantiomerically enriched chiral ligand.

      专利号:US-7119212-B2
      优先权日:2004-03-30
      标 题 :Process for the preparation of tolterodine and intermediates thereof
      发明人:COLOMBO LINO; ROSSI ROBERTO; ALLEGRINI PIETRO; CASTALDI GRAZIANO
      权利人:DIPHARMA SPA
      摘要:A process for the preparation of 6-methyl-4-(R)-phenyl-chroman-2-one and 6-methyl-4-(S)-phenyl-chroman-2-one, intermediates for the synthesis of tolterodine and its (S) enantiomer, by reaction of 6-methyl-coumarin with phenylboronic acids, esters and derivatives thereof, in the presence of chiral catalysts.

      专利号:US-2019185392-A1
      优先权日:2017-12-20
      标 题 :Carbon Dioxide as a Directing Group for C-H Functionalization Reactions Involving Lewis Basic Amines, Alcohols, Thiols, and Phosphines for the Synthesis of Compounds

      专利号:US-9751877-B2
      优先权日:2012-09-21
      标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
      发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
      权利人:PFIZER
      摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

      专利号:WO-2005005356-A2
      优先权日:2003-07-02
      标 题 :Enantioselective synthesis of enantiomerically enriched compounds

      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

      合成参考文献


      参考文献:10.1016/s0022-5347(06)00591-x
      摘要:Grocela JA, Kanji A, Ternullo J. Prediction of Medicare drug formulary drugs for treatment of overactive bladder. J Urol. 2006 Jul;176(1):252–5; discussion 255. doi: 10.1016/s0022-5347(06)00591-x.
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