CAS: 97205-34-0; Nebracetam

该化合物是属于赛马家族的化合物,以其认知增强特性著称,其特征是其结构上与Pirarestam相似,具有丙烯酮核心.Nebraxetam因其潜在的...

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MSDS等安全信息

    上下游产品

    N-Benzyl-5-Oxopyrrolidine-3-Methanol Methanesulfonate 1373821-40-9
    1-苄基-5-氧-3-吡咯烷羧酸甲酯 Methyl 1-Benzyl-5-Oxo-3-Pyrrolidinecarboxylate 51535-00-3
    4-Phthalimidomethyl-1-Benzyl-Pyrrolidin-2-One

    合成工艺路线路线简述

    • 合成目标产物 Nebracetam 主要起始原料 2-Pyrrolidinone, 4-[[(Methylsulfonyl)Oxy]Methyl]-1-(Phenylmethyl)-
    • (文献来源)合成步骤主要原料 2-Pyrrolidinone, 4-[[(Methylsulfonyl)Oxy]Methyl]-1-(Phenylmethyl)-
    📜N-Benzyl-5-Oxopyrrolidine-3-Methanol Methanesulfonate置于氨体系中,用 甲醇 作为反应溶剂,50.0 °C,500.01 Kpa 条件下,反应 8.0H,以94%的收率获得产物3,3'-二硝基联苯基-2,4'-二醇
    参考文献:一种奈拉西坦的制备方法
    标题:一种奈拉西坦的制备方法
    摘要:本发明公开了一种奈拉西坦的制备方法,属于药物化学技术领域.本发明的技术方案要点为:一种奈拉西坦的制备方法,以衣康酸二甲酯和苄胺为起始原料,经michael加成,分子内环合得1‑苄基‑5‑氧代吡咯烷‑3‑羧酸甲酯,1‑苄基‑5‑氧代吡咯烷‑3‑羧酸甲酯经硼氢化钠还原得1‑苄基‑4‑羟甲基‑吡咯烷‑2‑酮,1‑苄基‑4‑羟甲基‑吡咯烷‑2‑酮经甲磺酰化反应得1‑苄基‑5‑氧代吡咯烷‑3‑羧酸甲磺酸酯,最后1‑苄基‑5‑氧代吡咯烷‑3‑羧酸甲磺酸酯用氨水进行氨化还原即制得奈拉西坦.本发明制备过程简单,易于控制且目标产物收率较高,符合绿色化学的要求.

    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-7576211-B2
    优先权日:2004-09-30
    标题 :Synthesis of thienopyridinone compounds and related intermediates
    发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
    权利人:EPIX DELAWARE INC
    摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

    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:US-2009176740-A1
    优先权日:2007-11-30
    标题:Treatment of neurological conditions by the co-administration of aniracetam and l-alpha glycerylphosphorylcholine
    发明人:PHILLIPS II DAUGLAS JAMES
    权利人:PHILLIPS II DAUGLAS JAMES
    摘要:Aniracetam (1-[(4-methoxybenzoyl)]-2-pyrrolidinone) is co-administered with the acetylcholine precursor 1-alpha glycerylphosphorylcholine (Alpha GPC, choline alfoscerate, choline alphoscerate) to potentiate cognition enhancing effects in healthy subjects and patients suffering from neurological conditions including Alzheimer's Disease (AD), attention deficit disorder (ADD), Parkinson's Disease, schizophrenia, vascular dementia, post stroke aphasia, anxiety disorders, cerebral atrophy, chronic alcoholism, Down syndrome, dyslexia, and various other neurodegenerative conditions. The co-administration of aniracetam (and other racetam derivatives including oxiracetam) with the acetylcholine precursor 1-alpha glycerylphosphorylcholine decreases negative side-effects such as severe headaches while increasing the synthesis and release of the neurotransmitters acetylcholine and glutamate to facilitate proper brain functioning.

    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

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Ma J, Lin J, Zhao L, Harms K, Marsch M, Xie X, Meggers E. Synthesis of beta-Substituted gamma-Aminobutyric Acid Derivatives via Enantioselective Photoredox Catalysis. Angew Chem Int Ed Engl. 2018 Apr 30. doi: 10.1002/anie.201804040. [Epub ahead of print] doi: 10.1016/j.jsurg.2007.08.009.
    5: Takeo S, Hayashi H, Tadokoro M, Takagi K, Miyake K, Takagi N, Oshikawa S. Effects of nebracetam on synaptosomal monoamine uptake of striatal and hippocampal regions in rats. Biol Pharm Bull. 1997 Apr;20(4):360-3. Review.

    合成参考文献


    参考文献:10.1016/s0021-5198(19)39754-9|10.1254/jjp.58.117
    摘要:Iwasaki K, Matsumoto Y, Fujiwara M. Effect of Nebracetam on the Disruption of Spatial Cognition in Rats. Japanese Journal of Pharmacology. 1992;58(2):117–26. doi: 10.1016/s0021-5198(19)39754-9.
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