CAS: 675126-08-6; Dasotraline Hydrochloride

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上下游产品

(1R,4S)-N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-naphthalen-1-yl]-formamide N-((1S,4R)-1-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-4-yl)acetamide (4S)-4-(3,4-dichlorophenyl)-1-tetralone N-((1S,4R)-1-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-4-yl)acetamide

合成工艺路线路线简述

    📜4-(3,4-二氯苯基)-1-四氢萘酮置于甲醇,Sodium Tetrahydroborate,三氟乙酸体系中,用 甲苯 作为反应溶剂,化学反应 74.5H,反应生成 (1R,4S)-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺盐酸盐(1:1)
    参考文献:Processes For The Preparation Of Dasotraline And Intermediates Thereof
    标题:Processes For The Preparation Of Dasotraline And Intermediates Thereof
    摘要:本发明提供了制备dasotraline(1)的工艺,以及在制备中有用的中间体.具体而言,提供了用于生产化合物formula(2)或其盐的工艺,以及其去保护以得到dasotraline(1)的工艺.

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    专利信息


    专利号:EP-3800178-A1
    优先权日:2019-10-01
    标题:Preparation of enamide intermediate for the synthesis of dasotraline
    发明人:BALLETTE ROBERTO; DOBARRO RODRÃ?GUEZ ALICIA
    权利人:MOEHS IBERICA SL
    摘要:The present invention relates to a process for the preparation of N -(( S )-4-(3,4-dichlorophenyl)-3,4-dihydronaphthalen-1-yl)acetamide, which is a suitable intermediate for the synthesis of dasotraline or a pharmaceutically acceptable salt thereof, as well as to a process for the preparation of dasotraline or a pharmaceutically acceptable salt thereof using said N -(( S )-4-(3,4-dichlorophenyl)-3,4-dihydronaphthalen-1-yl)acetamide intermediate.

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    主要参考文献


    1: Koblan KS, Hopkins SC, Sarma K, Gallina N, Jin F, Levy-Cooperman N, Schoedel KA, Loebel A. Assessment of human abuse potential of dasotraline compared to methylphenidate and placebo in recreational stimulant users. Drug Alcohol Depend. 2016 Feb 1;159:26-34. doi: 10.1016/j.drugalcdep.2015.10.029. Epub 2015 Dec 3. doi: 10.1038/npp.2015.124. Epub 2015 May 7.

    合成参考文献

    参考DOI号:10.1002/chem.200802303
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