CAS: 147116-67-4; (2S,3S)-2-Benzhydryl-N-(5-(Tert-Butyl)-2-Methoxybenzyl)Quinuclidin-3-Amine

结构式图片

欧盟法规

REACH注册C&L通报

上下游产品

(2-Diphenylmethyl-1-Azabicyclo[2.2.2]Oct-3-yl)-Benzylamine 155681-48-4
(-)-(2S,3S)-Cis-2-(Diphenylmethyl)-1-Azabicyclo[2.2.2]Octane-3-Amine 142035-23-2
(+)-(2S,3R)-2-(Diphenylmethyl)-1-Azabicyclo<2.2.2>Octan-3-Ol
(S)-2-Diphenylmethylquinuclidin-3-One 683206-53-3

合成工艺路线路线简述

  • 合成目标产物 (2S,3S)-2-Benzhydryl-N-(5-Tert-Butyl-2-Methoxybenzyl)Quinuclidin-3-Amine 主要起始原料 Benzene, 2-(Bromomethyl)-4-(1,1-Dimethylethyl)-1-Methoxy- And 1-Azabicyclo[2.2.2]Octan-3-Amine, 2-(Diphenylmethyl)-, (2S,3S)-
  • (文献来源)合成步骤主要原料 Benzene, 2-(Bromomethyl)-4-(1,1-Dimethylethyl)-1-Methoxy- 和 1-Azabicyclo[2.2.2]Octan-3-Amine, 2-(Diphenylmethyl)-, (2S,3S)-
(2S,3S)-2-Diphenylmethyl-N-((S)-1-Phenylethyl)Quinuclidin-3-Amine置于4-二甲氨基吡啶,5%-Palladium/activated Carbon,氢气,三乙胺体系中,用 N,N-二甲基甲酰胺,异丙醇 用作溶剂,化学反应 24.0H,反应生成马罗匹坦
参考文献:制备马罗匹坦游离碱的方法
标题:制备马罗匹坦游离碱的方法
摘要:本发明涉及马罗匹坦游离碱的制备方法,反应式如下:.

海关参考信息

专利信息


专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:EP-1713801-B1
优先权日:2004-02-02
标 题:Process for preparation of 1-(2s,3s)-2-benzhydr yl-n-(5-tert-butyl-2-methoxybenzyl)quinuclidin-3-amine
发明人:BASFORD PATRICIA ANN; POST RONALD JAMES; SMITH JULIAN DUNCAN; TABER GERALDINE PATRICIA
权利人:PFIZER PROD INC
摘要:This invention relates to an improved process for the preparation of (2S,3S)-­ 2-benzhydryl-N-(5-tent-butyl-2-methoxybenzyl)quinuclidin-3-amine, (hereinafter 'compound of Formula I') and its pharmaceutically acceptable salts. In particular, the invention is directed to an improved synthesis of the monohydrate citrate salt of the compound of Formula (la).

专利号:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:US-2005222431-A1
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-7227028-B2
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
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主要参考文献


1: Myers J, Voges A, Werner R, Ritter N. Maropitant Citrate Administration Significantly Decreases the Rate of Peristalsis in the Stomach and Jejunum and Does Not Significantly Alter Intestinal Diameter or Intestinal Wall Thickness in Healthy Adult Dogs. Vet Radiol Ultrasound. 2026 May;67(3):e70167. doi: 10.1111/vru.70167. 90(2):59-64.
3: Gould AG, Akucewich LH, Thomas RC, Lewis ST, Ghubash R. Influence of Maropitant Citrate on Pollen and Control Intradermal Test Reactivity in Atopic Dogs: A Randomised, Controlled, Blinded Trial. Vet Dermatol. 2025 Dec 25. doi: 10.1111/vde.70045. Epub ahead of print. 50(1):17. doi: 10.1007/s11259-025-10966-8. 35(3):197-206. doi: 10.1111/vec.13476. Epub 2025 Jun 16. 86(7):ajvr.25.02.0040. doi: 10.2460/ajvr.25.02.0040. 27(2):1098612X241309826. doi: 10.1177/1098612X241309826.
9: Gölgeli Bedir A, Yanmaz LE, Okur S, Şenocak MG, Turgut F, Kocaman Y, Orhun ÖT, Ersöz U, Baykal B. The Effect of Maropitant, Ondansetron and Metoclopramide on Dexmedetomidine-Induced Vomiting in Cats. Vet Med Sci. 2025 Jan;11(1):e70152. doi: 10.1002/vms3.70152.

合成参考文献


参考文献:10.2460/javma.21.02.0082
摘要:Burke JE, Hess RS, Silverstein DC. Effectiveness of orally administered maropitant and ondansetron in preventing preoperative emesis and nausea in healthy dogs premedicated with a combination of hydromorphone, acepromazine, and glycopyrrolate. J Am Vet Med Assoc. 2021 Dec 15;260(S1):S40–5. doi: 10.2460/javma.21.02.0082.
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