CAS: 46817-91-8; 2-((2-Ethoxyphenoxy)Methyl)Morpholine

该化合物是一种化学化合物,主要被确认为用于药物,特别是治疗注意力-缺损/高活性紊乱(ADHD),被归类为选择性的无肾上腺素再摄入抑制剂(NRI),并显示其可调节大脑...

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CAS号35604-67-2 2-[(2-乙氧基苯氧基)甲基... | CAS号94-71-3 邻乙氧基苯酚 | CAS号40987-25-5 4-苄基-2-氯甲基吗啡啉 | CAS号5296-35-5 2-乙氧基苯基缩水甘油醚 | CAS号926-39-6 2-氨基乙醇硫酸氢酯

合成工艺路线路线简述

    📜(+/-)-4-Benzyl-2-(2-Ethoxyphenoxymethyl)Morpholine置于palladium On Activated Charcoal 盐酸,氢气体系中,用 乙醇 作为反应溶剂,以96%的收率获得产物维洛沙秦
    参考文献:作为多巴胺d4受体配体的新系列吗啉和1,4-恶唑烷衍生物:合成和3D-Qsar模型.
    标题:作为多巴胺d4受体配体的新系列吗啉和1,4-恶唑烷衍生物:合成和3D-Qsar模型.
    摘要:自多巴胺d(4)受体亚型的鉴定和关于其可能参与精神分裂症的推测以来,选择性d(4)配体的开发已投入大量工作.这些选择性配体可能是没有锥体束外副作用的有效抗精神病药.这项工作描述了对多巴胺d(4)受体具有选择性的新系列的2,4-二取代的吗啉和2,4-二取代的1,4-恶唑酮的合成.进行了使用grid / Golpe方法的3D-Qsar分析,目的是更好地了解化学结构与生物活性之间的关系.通过查看系数图,我们可以确定对于亲和力至关重要的区域位于两个苯环系统(对氯苄基)周围,和属于吗啉或1,4-氧杂庚烷体系的脂族胺.另外,吗啉或1,4-氧杂庚烷环的大小对于亲和力似乎很重要.
    DOI:10.1021/jm031111M

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    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-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:US-7309799-B2
    优先权日:2004-06-01
    标 题:Methods for the synthesis of milnacipran and congeners thereof
    发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
    权利人:COLLEGIUM PHARMACEUTICAL INC
    摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

    专利号:US-9884844-B2
    优先权日:2012-12-31
    标 题:Heterocyclic compounds and methods of use thereof
    发明人:FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L
    权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC
    摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Findling RL, Katic A, Liebowitz M, Waxmonsky J, Fry N, Qin P, Yarullina I, Maldonado-Cruz Z, Lieberman VR, Rubin J. Viloxazine Extended-Release Capsules in Children and Adolescents with Attention-Deficit/Hyperactivity Disorder: Results of a Long-Term, Phase 3, Open-Label Extension Trial. CNS Drugs. 2025 Aug 13. doi: 10.1007/s40263-025-01209-0. Epub ahead of print. 15(1):28919. doi: 10.1038/s41598-025-14385-2.
    3: Maneeton P, Maneeton B, Winichaikul Y, Kawilapat S, Kienngam N, Maneeton N. Efficacy and Tolerability of Viloxazine Compared to Placebo on Emotional, Behavioral, and Executive Functioning in Children and Adolescents with ADHD: A Systematic Review and Meta-Analysis. Neuropsychiatr Dis Treat. 2025 May 12;21:1029-1045. doi: 10.2147/NDT.S494229.
    4: Aishah A, Kim M, Gell L, Vena D, Azarbarzin A, Pho H, Norman D, Ojile J, Esmaeili N, Taranto-Montemurro L, Wellman A, Sands S, Messineo L. Effect of viloxazine and trazodone in obstructive sleep apnoea: a randomised, placebo- controlled, cross-over study. Thorax. 2025 Aug 15;80(9):641-649. doi: 10.1136/thorax-2024-222513.

    合成参考文献


    摘要:Handbook of Experimental Pharmacology., 55(527), 1980
    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
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