(R)-托特罗定l-酒石酸盐置于碳酸氢钠体系中,用 乙酸乙酯 用作溶剂,以6.9 G的收率获得托特罗定 参考文献: 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[fr] Nouveau (R) Et 3-(2-(Allyloxy)-5-Méthylphényl)-N,N-Diisopropyl-3-Phénylpropan-1-Amine Racémique Et Son Utilisation Pour La Synthèse De (R) Et De 2-(3-(Diisopropylamino)-1-Phénylpropyl)-4-(Hydroxyméthyl)Phénol Racémique 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[fr] Nouveau (R) Et 3-(2-(Allyloxy)-5-Méthylphényl)-N,N-Diisopropyl-3-Phénylpropan-1-Amine Racémique Et Son Utilisation Pour La Synthèse De (R) Et De 2-(3-(Diisopropylamino)-1-Phénylpropyl)-4-(Hydroxyméthyl)Phénol Racémique 摘要:本发明涉及新颖的手性3-(2-(烯丙氧基)-5-甲基苯基)-N,N-二异丙基-3-苯丙胺(5)和消旋3-(2-(烯丙氧基)-5-甲基苯基)-N,N-二异丙基-3-苯丙胺()以及其在改进和工业上有利的制备手性和消旋形式2-(3-(二异丙胺基)-1-苯基丙基)-4-(羟甲基)苯酚的过程中的使用.此外,本发明还涉及其制备.
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:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
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-8299306-B2 优先权日:2006-06-08 标 题 :Accelerated synthesis of substituted hydroxymethyl phenols 发明人:ENNIS SETH C; KENNEDY BRYAN D 权利人:ENNIS SETH C; KENNEDY BRYAN D 摘要:This disclosure relates to process for the preparation of a compound of formula (I) wherein R is hydrogen, a straight or branched C 1 -C 6 alkyl-carbonyl group or a phenylcarbonyl group, or a salt thereof, comprising the following steps: a) adding to a suspension of Mg a compound of formula (II) R 1 (MgX) n —LiY wherein n is 1 or 2; R 1 is an aromatic, aliphatic, carbocyclic or heterocyclic organic group having 1 to 24 carbon atoms; X and Y are independently selected from Cl, Br and I, b) reacting said reaction mixture with a suitable halogenated compound in a solvent to form a Grignard reagent, c) reacting said Grignard reagent with a suitable linear, branched or cyclic carbonate to obtain a compound of formula (IV) wherein A is a linear, branched or cyclic C 1 -C 6 alkyl group, and preferably a methyl group, and then further reacting the compound of formula (IV) in a known manner to obtain a compound of formula (I) and optionally salt formation.
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-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
1: Gacci M, Sebastianelli A, Salvi M, Schiavina R, Brunocilla E, Novara G, De Nunzio C, Tubaro A, Oelke M, Gravas S, Carini M, Serni S. Tolterodine in the Treatment of Male LUTS. Curr Urol Rep. 2015 Sep;16(9):60. doi: 10.1007/s11934-015-0531-9. Review. doi: 10.1186/1471-2490-14-84. Review. 3: Angulo JC, Valpas A, Rejas J, Linden K, Kvasz M, Snedecor SJ. Cost effectiveness of fesoterodine and tolterodine for the treatment of overactive bladder with urge urinary incontinence in Spain and Finland. Clin Drug Investig. 2014 May;34(5):297-307. doi: 10.1007/s40261-014-0178-1. Review. Review. doi: 10.1517/14656566.2013.823158. Epub 2013 Jul 26. Review. doi: 10.2147/OAJU.S7232. Review. 7: Chung DE, Te AE. Tolterodine extended-release for overactive bladder. Expert Opin Pharmacother. 2009 Sep;10(13):2181-94. doi: 10.1517/14656560903167965. Review. Review. Epub 2009 May 14. Review.
合成参考文献
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