CAS: 197010-20-1; 2-((1-Benzylpiperidin-4-yl)(Hydroxy)Methyl)-5,6-Dimethoxy-2,3-Dihydro-1H-Inden-1-One

该化合物是Donepezil的衍生物,这是主要用于治疗阿尔茨海默氏病的著名乙酰胆碱酯酶抑制剂,该化合物的特征是增强药理特性的氢氧基组. Donepezil 的特征是,它有能力通过提高脑中对记忆和学习至关重要的乙酰胆碱水平来提高认知功能.分子结构通常包括双环芳香系统,有助于其亲热性和跨越血脑屏障的能力.它通常溶于有机溶剂,在生理条件下具有中等稳定性.该化合物的功效和安全特征是正在进行的研究的主题,特别是其潜在的...

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1-benzyl-4-(5,6-dimethoxy-1-oxo-indane-2-carbonyl)-pyridinium chloride donepezil piperidine1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenyl)methylpiperidine

合成工艺路线路线简述

    多奈哌齐杂质置于platinum On Activated Charcoal 氢气,碳酸氢钠体系中,用 甲醇,水 用作溶剂,20.0 °C,600.01 Kpa 条件下,反应生成羟基多萘哌齐
    参考文献:Wo2007/15052
    标题:Wo2007/15052

    海关参考信息

    专利信息


    专利号:US-2009253746-A1
    优先权日:2005-11-14
    标题 :Synthesis and Preparations of Intermediates and New Polymorphs Thereof Useful For The Preparation Of Donepezil Hydrochlcoride
    发明人:SOLDEVILLA MADRID NURIA
    权利人:SOLDEVILLA MADRID NURIA
    摘要:The invention relates to an improved process for preparing 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyin-dan- 1 -one (a key intermediate in the synthesis of donepezil hydrochloride), crystalline polymorph forms of this key intermediate and their use thereof for producing donepezil hydrochloride. In particular, the invention provides an improved method for producing the intermediate 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyindan-1-one. The process includes reacting 5,6-dimethoxyin-dan- 1 -one with 1-benzylpiperidine-4-carbaldehyde using potassium hydroxide in an aqueous solvent. The aqueous solvent can be a mixture of an organic solvent and water Where the organic solvent is not miscible with water, the reaction may be performed in the presence of a phase transfer catalyst.

    专利号:US-2009298879-A1
    优先权日:2006-05-18
    标 题 :Impurities of Donepezil
    发明人:KRIZMANIC IRENA; LERMAN LIDIJA; SAMARDZIC ZRINKA; KACZOROWSKA KATARZYNA; MANIKOWSKI ANDRZEJ; ZIORO BARBARA; GREBENAR IVICA; KORUZNJAK JASNA DOGAN
    权利人:PLIVA HRVATSKA D O O
    摘要:The present invention relates to impurities of donepezil, or a pharmaceutically acceptable salt thereof, which may be produced during synthesis and storage of donepezil, or a pharmaceutically-acceptable salt thereof, and to methods of identifying such impurities. The invention also relates to the use of these impurities in analytical techniques and to product that contain certain low levels of these impurities in particular the following impurities are disclosed: formula (I) and formula (II).

    专利号:EP-1960357-A2
    优先权日:2005-11-14
    标 题 :Synthesis and preparations of intermediates and polymorphs thereof useful for the preparation of donepezil hydrochloride

    专利号:CA-2629720-A1
    优先权日:2005-11-14
    标 题:Synthesis and preparations of intermediates and polymorphs thereof useful for the preparation of donepezil hydrochloride

    专利号:JP-2009515945-A
    优先权日:2005-11-14
    标题 :Improved synthesis and preparation of intermediates and novel polymorphs useful for the preparation of donepezil hydrochloride

    专利号:WO-2007119118-A2
    优先权日:2005-11-14
    标题 :Synthesis and preparations of intermediates and polymorphs thereof useful for the preparation of donepezil hydrochloride
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