CAS: 27591-69-1; 2,7-Bis(2-(Diethylamino)Ethoxy)-9H-Fluoren-9-One Dihydrochloride

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CAS号27591-97-5 替洛隆 | CAS号869-24-9 2-二乙氨基氯乙烷盐酸盐 | CAS号100-37-8 二乙氨基乙醇 | CAS号67-63-0 异丙醇 | CAS号27591-97-5 替洛隆 | CAS号93418-47-4 2-[7-[2-(diethy...

乙胺芴酮 在 盐酸体系中,用 乙醇作为反应溶剂,以200 G的收率获得tilorone DihydroChloride
参考文献:一种具有明显的ifn-α诱导活性的盐酸双氯隆的有效合成方法.
标题:一种具有明显的ifn-α诱导活性的盐酸双氯隆的有效合成方法.
摘要:盐酸噻氯隆(1)具有诱导干扰素抵抗病原体感染的巨大潜力.在本文中,我们描述了一种方便的制备2,7-二羟基芴-9-一(2)的方法,这是制备替洛龙二盐酸盐(1)的常用药物中间体.在该新方法中,在较温和的条件下以较高的收率进行了4,4'-二羟基-[1,1'-联苯]-2-羧酸的甲基酯化反应(4),这在化合物的制备中起着重要作用2.通过熔点,Ir,Ms和1 H-Nmr表征相关中间体和目标化合物的结构.此外,合成的盐酸氢吡咯酮在12 H内对小鼠干扰素-α(Ifn-α)的诱导具有明显的作用,直至24 H观察到峰值.
Doi:10.3390/Molecules201219781

专利信息

专利号:US-2024409495-A1
优先权日:2021-10-20
标 题 :Process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts
发明人：JAISANKAR PARASURAMAN; DEB INDUBHUSAN; BHATTACHARJEE PINAKI
权利人:COUNCIL SCIENT IND RES
摘要:Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.

专利号:WO-2025076406-A1
优先权日:2023-10-05
标题:Synthesis and evaluation of 9-aminoacridines with sars-cov-2 antiviral activity
发明人：JONES THANE; LANE THOMAS; MAKAROV VADIM; EKLINS SEAN
权利人:COLLABORATIONS PHARMACEUTICALS INC
摘要:The synthesis and characterization of a series of derivatives and analogs based on the 9-aminoacridine scaffold shared by antimalarial drugs quinacrine and pyronaridine are described. Also described is the structure-activity relationship of these compounds against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus that causes the coronavirus disease of 2019 (COVID-19). Several compounds displayed potent in vitro activity, with 50% inhibitory concentrations below 1 micromolar.

专利号:US-2009012088-A1
优先权日:2005-07-26
标 题:Compounds for the Treatment of Neurodegeneration and Stroke
发明人：HERGENROTHER PAUL J; PUTT KARSON S; LIU XIANJUN
权利人:HERGENROTHER PAUL J; PUTT KARSON S; LIU XIANJUN
摘要:Compounds and related methods for synthesis, and the use of compounds for the treatment of neurodegenerative diseases are disclosed. Compounds are disclosed in connection with PARG and/or PARP inhibition. Therapeutic applications are relevant for preventing or inhibiting neurological cell death for a variety of neurodegenerative conditions including Parkinson's disease, ischemia, and stroke. Also disclosed is a high-throughput screen for identifying compounds capable of inhibiting PARG and/or PARP.

专利号:WO-2023067624-A1
优先权日:2021-10-20
标 题 :A process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts

专利号:WO-2009056955-A1
优先权日:2007-10-30
标题 :Amine-bearing phospholipids (abps), their synthesis and use
发明人：ZUMBUEHL ANDREAS
权利人:UNIV BASEL; ZUMBUEHL ANDREAS
摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

专利号:CN-118175999-A
优先权日:2021-10-20
标题 :Process for the preparation of 2, 7-dihydroxy-9-fluorenone useful for the synthesis of telulone and its salts