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里特反应介导的新型金刚烷胺类似物2-氧杂金刚烷-5-胺的合成。

Ritter reaction-mediated syntheses of 2-oxaadamantan-5-amine, a novel amantadine analog.

作者信息

Leiva Rosana, Gazzarrini Sabrina, Esplugas Roser, Moroni Anna, Naesens Lieve, Sureda Francesc X, Vázquez Santiago

机构信息

Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII, s/n, Barcelona E-08028, Spain.

Department of Biosciences and National Research Council (CNR) Biophysics Institute (IBF), University of Milan, Via Celoria 26, 20133 Milan, Italy.

出版信息

Tetrahedron Lett. 2015 Mar 4;56(10):1272-1275. doi: 10.1016/j.tetlet.2015.01.160. Epub 2015 Jan 31.

Abstract

Two alternative syntheses of 2-oxaadamantan-5-amine, a novel analog of the clinically approved drug amantadine, are reported. The compound has been tested as an anti-influenza A virus agent and as an NMDA receptor antagonist. While the compound was not antivirally active, it displayed moderate activity as an NMDA receptor antagonist.

摘要

报道了2-氧杂金刚烷-5-胺的两种替代合成方法,它是临床批准药物金刚烷胺的一种新型类似物。该化合物已作为抗甲型流感病毒剂和N-甲基-D-天冬氨酸(NMDA)受体拮抗剂进行了测试。虽然该化合物没有抗病毒活性,但它作为NMDA受体拮抗剂表现出中等活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7188/7125674/13cd5a09dbd1/fx1_lrg.jpg

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