CAS: 207679-81-0; 5-Hydroxymethyl Tolterodine

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(R)-[4-Benzyloxy-3-(3-Diisopropylamino-1-Phenyl-Propyl)-Phenyl]-Methanol Fumarate置于raney Nickel Sodium Carbonate,Sodium Hydroxide,氢气体系中,用 二氯甲烷,水,甲醇 用作溶剂,以59%的收率获得(R)-5-羟甲基托特罗定
参考文献: A Process For Preparing Fesoterodine[fr] Procédé De Préparation De Fésotérodine
标题: A Process For Preparing Fesoterodine[fr] Procédé De Préparation De Fésotérodine
摘要:本发明涉及一种改进的制备fesoterodine及其药用盐的方法.本发明特别涉及一种制备fesoterodine及其药用盐的方法,其中涉及使用和制备r(+)苄基托特罗定和r(+)-[4-苄氧基-3-(3-二异丙基氨基-1-苯基丙基)-苯基]-甲醇富马酸盐.

专利信息

专利号:WO-2017137955-A1
优先权日:2016-02-14
标题:Novel (r) and rac 3-(2-(allyloxy)-5-methylphenyl)-n,n-diisopropyl-3- phenylpropan-1-amine and its use for synthesis of (r) and rac-2-(3- (diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol
发明人：THOMBARE PRAVIN SAHADEV
权利人:CELESTIS PHARMACEUTICALS PVT LTD
摘要:The present invention relates to novel chiral 3-(2-(allyloxy)-5-methylphenyl)-N,N-diisopropyl-3-phenylpropan-1-amine (5) and racemic 3-(2-(allyloxy)-5-methylphenyl)-N,N-diisopropyl-3-phenylpropan-1-amine () and its use in improved and industrially advantageous process for preparation of chiral and racemic form of 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol. Further, present invention relates to preparation of the same.

专利号:EP-1862449-A1
优先权日:2006-05-31
标 题 :A shortened synthesis of substituted hydroxymethyl phenols
发明人：BROWNE ROISIN; KIKELLY MICHAEL
权利人:SCHWARZ PHARMA LTD
摘要:The present disclosure relates to a process for the preparation of 2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol or its phenolic monoesters or salts thereof, characterized by the steps of na) reacting a compound of formula (II)n nwith a mixture of MeMgCl and Mg in a solvent, nb) optionally reducing the temperature of the Grignard reagent to a lower temperature than in step a), and n nreacting the resulting Grignard reagent with an excess of a carbonate in a solvent, to obtain a compound of formula (III)n nwherein A is a C 1 -C 6 alkyl group, and then further reacting the compound of formula (III) in a known manner to obtain the desired end product.

专利号:US-8703996-B2
优先权日:2010-03-09
标题:Short synthesis of tolterodin, intermediates and metabolites
发明人：STERK DAMJAN
权利人:STERK DAMJAN; LEK PHARMACEUTICALS
摘要:A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.

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:US-6809214-B2
优先权日:2000-06-14
标 题 :Shortened synthesis of 3,3-diarylpropylamine derivatives
发明人：MEESE CLAUS O
权利人:SANOL ARZNEI SCHWARZ GMBH
摘要:The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.

专利号:US-8344176-B2
优先权日:2006-05-31
标 题 :Synthesis of substituted hydroxymethyl phenols
发明人：BROWNE ROISIN; KILKELLY MICHAEL
权利人:SCHWARZ PHARMA LTD; BROWNE ROISIN; KILKELLY MICHAEL
摘要:The present disclosure relates to a process for the preparation of 2-(3 -diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol or its phenolic monoesters or salts thereof, characterized by the steps of a) reacting a compound of formula (II) with a mixture of a Grignard initiator and Mg in a solvent; b) optionally reducing the temperature of the Grignard reagent to a lower temperature than in step a), and reacting the resulting Grignard reagent with an excess of a carbonate in a solvent, to obtain a compound of formula (III) wherein A is a C 1 -C 6 alkyl, and the further reacting the compound of formula (III) in a known manner to obtain the desired end product.