CAS: 140148-70-5; (S)-1-Boc-Pyrrolidine-3-Carboxylic Acid

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合成工艺路线路线简述

    1-Boc-吡咯烷-3-甲酸甲酯置于水,Potassium Carbonate,Lithium Hydroxide体系中,用 四氢呋喃,Aq. Phosphate Buffer 用作溶剂,化学反应生成(S)-1-Boc-吡咯烷-3-甲酸
    参考文献:Discovery Of A Potent,Dual Serotonin And Norepinephrine Reuptake Inhibitor
    标题:Discovery Of A Potent,Dual Serotonin And Norepinephrine Reuptake Inhibitor
    摘要:The Objective Of The Described Research Effort Was To Identify Novel Serotonin And Norepinephrine Reuptake Inhibitor (Snri) With Improved Norepinephrine Transporter Activity And Acceptable Metabolic Stability And Exhibiting Minimal Drug-Drug Interaction. We Describe Herein The Discovery Of A Series Of 3-Substituted Pyrrolidines Exemplified By Compound 1. Compound 1 Is A Selective Snri In Vitro And In Vivo Has Favorable Adme Properties,And Retains Inhibitory Activity In The Formalin Model Of Pain Behavior. Compound 1 Thus Represents A Potential New Probe To Explore Utility Of Snris In Central Nervous System Disorders,Including,Chronic: Pain Conditions.
    Doi:10.1021/ml400049P

    海关参考信息

    专利信息


    专利号:EP-1836163-B1
    优先权日:2004-12-23
    标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
    发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
    权利人:NOVARTIS AG
    摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
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    合成参考文献


    参考文献:10.1055/s-0028-1087965
    摘要:Lee H, Medda A. 3,4-Methano-β-Proline: A Conformationally Constrained β-Amino Acid. Synlett. 2009 Mar 16;2009(06):921–4. doi: 10.1055/s-0028-1087965.
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