CAS: 69559-11-1; 2-((4-Aminopentyl)(Ethyl)Amino)Ethanol

上下游产品

CAS号74509-79-8 5-[乙基(2-羟乙基)氨基]-2-戊酮

α-乙酰基-γ-丁内酯置于氢碘酸,氢气,羟胺,Potassium Carbonate体系中,用 四氢呋喃,水 作为反应溶剂,80.0~100.0 °C,1.0 Mpa 条件下,反应 4.42H,反应生成 5-(N-乙基-N-2-羟乙基胺)-2-戊胺
参考文献:高产连续流合成抗疟药羟氯喹.
标题:高产连续流合成抗疟药羟氯喹.
摘要:近年来,已经报道了许多用于连续制备精细化学品和药物活性成分(api'S)的合成方法,从而极大地提高了工艺效率.在此,我们报告了抗疟药物羟氯喹(hcq)的高效连续合成.新工艺的关键改进包括消除了保护基,与目前的商业工艺相比,总收率提高了52%.连续方法采用填充床反应器与连续搅拌釜反应器的组合,以将起始原料直接转化为产物.这种高产,数克级的连续合成提供了一个机会,可以增加全球对羟基氯喹的治疗途径.
DOI:10.3762/bjoc.14.45

专利信息

专利号:US-12071410-B2
优先权日:2018-02-26
标 题:High-yielding continuous flow synthesis of antimalarial drug hydroxychloroquine
发明人：GUPTON FRANK B; AHMAD SAEED; GUNURU HARI P R; TELANG NAKUL S
权利人:UNIV VIRGINIA COMMONWEALTH
摘要:Cost effective, semi-continuous flow methods and systems for synthesizing the antimalarial drug hydroxychloroquine (HCQ) in high yield are provided. The synthesis method that uses simple, inexpensive reagents to obtain the crucial intermediate 5-(ethyl(2-hydroxyethyl)-amino)pentan-2-one, vertical-integration of the starting material 5-iodopentan-2-one and the integration of continuous stirred tank reactors.

专利号:WO-2019165337-A1
优先权日:2018-02-26
标 题:High-yielding continuous flow synthesis of antimalarial drug hydroxychloroquine

专利号:WO-2024261606-A1
优先权日:2023-06-22
标 题:Production process for hydroxychloroquine under concentrated conditions
发明人：ERTÃœRK ERKAN; BALOÄžLU HALIT
权利人:TUEBITAK
摘要:The present invention discloses an improved, practical and solvent-accelareted process for the synthesis of hydroxychloroquine by the reaction of 4,7- dichloroquinoline and 2-[(4-aminopentyl)(ethyl)amino]ethanol under concentrated conditions.

专利号:US-2020407321-A1
优先权日:2018-02-26
标 题:High-yielding continuous flow synthesis of antimalarial drug hydroxychloroquine

专利号:CN-114057640-A
优先权日:2020-08-05
标 题 :A kind of asymmetric synthesis method of optically pure (R)/(S)-hydroxychloroquine side chain

专利号:CN-105693606-A
优先权日:2016-03-09
标题:A kind of asymmetric synthesis method of optically pure (R)/(S)-hydroxychloroquine