Preparation method of (3R,4R)-(1-benzyl-4-methylpiperidine-3-yl)methylamine-L-di-p-toluoyltartaric acid salt

一种(3r,4r)-(1-苄基-4-甲基哌啶-3-基)甲胺-l-二对甲苯甲酰酒石酸盐的制备方法

  • Inventors: LIU WEIGUO
  • Assignees: 刘卫国
  • Publication Date: January 13, 2016
  • Publication Number: CN-105237463-A

Abstract

The invention discloses a preparation method of (3R,4R)-(1-benzyl-4-methylpiperidine-3-yl)methylamine-L-di-p-toluoyltartaric acid salt prepared from the following reaction steps shown in the description. The preparation method of (3R,4R)-(1-benzyl-4-methylpiperidine-3-yl)methylamine-L-di-p-toluoyltartaric acid salt has the following advantages that the process is novel in design, extremely dangerous chemicals (such as lithium aluminum hydride) are not required to be used, a folding condensation process is adopted, and the total yield is high; more importantly, the starting materials are cheap and easy to obtain, and the cost is low; and the maneuverability is high, and industrialization is easy.
本发明公开一种(3R,4R)-(1-苄基-4-甲基哌啶-3-基)甲胺-L-二对甲苯甲酰酒石酸盐的制备方法,由以下反应步骤制得:本发明提供的(3R,4R)-(1-苄基-4-甲基哌啶-3-基)甲胺-L-二对甲苯甲酰酒石酸盐的制备方法,具有如下优势:本发明工艺设计新颖,不需要使用很危险的化学品(如:四氢铝锂),采用叠缩工艺,总收率高;更重要的是,起始物料便宜易得,成本低;可操作性强,易于工业化。

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Patent Citations (5)

    Publication numberPublication dateAssigneeTitle
    CN-103896826-AJuly 02, 2014上海朴颐化学科技有限公司Asymmetric synthesis method of nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine, and relevant intermediate and raw material preparation method
    CN-104837817-AAugust 12, 2015力奇制药公司制备3-氨基-哌啶化合物的新合成路线
    CN-104860872-AAugust 26, 2015天津药物研究院有限公司Bis-(3R,4R)-1-benzyl-N,4-dimethyl piperidin-3-amine L-di-p-toluyl tartrate synthesis method
    JP-2011236157-ANovember 24, 2011Toray Fine Chemicals Co Ltd, 東レ・ファインケミカル株式会社Method for producing optically active nipecotic acid derivative
    WO-2015087201-A1June 18, 2015Unichem Laboratories LimitedProcede ameliore pour la preparation de (3r,4r)-(1-benzyl-4-methylpiperidin-3yl)-methylamine

NO-Patent Citations (3)

    Title
    BRIAN R. DE COSTA等: "Synthesis and Biological Evaluation of Conformationally Restricted 2-(l -Pyrrolidinyl)-N-[2-(3 ,4-dichlorophenyl)ethyl]-N-mehty lethylenediamines as a Receptor Ligands. 1. Pyrrolidine, Piperidine, Homopiperidine, and Tetrahydroisoquinoline Classes", 《JOURNAL OF THE MEDICINAL CHEMISTRY》
    DAVID H. BROWN RIPIN等: "Development of a Scaleable Route for the Production of cis-N-Benzyl-3-methylamino-4-methylpiperidine", 《ORGANIC PROCESS RESEARCH & DEVELOPMENT》
    张从海,等: "伯胺的单烷基化反应研究进展", 《化学研究与应用》

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    Publication numberPublication dateAssigneeTitle