会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 48. 发明申请
    • NOVEL METHOD FOR PREPARATION OF ATOVAQUONE
    • 用于制备大田的新方法
    • WO2012153162A1
    • 2012-11-15
    • PCT/IB2011/001507
    • 2011-06-28
    • LUPIN LIMITEDROY, Bhairab, NathSINGH, Girij, PalLATHI, Piyush, SureshAGRAWAL, Manoj, KunjabihariMITRA, RanganTRIVEDI, Anurag
    • ROY, Bhairab, NathSINGH, Girij, PalLATHI, Piyush, SureshAGRAWAL, Manoj, KunjabihariMITRA, RanganTRIVEDI, Anurag
    • C07C46/00C07C49/403C07C49/427C07C50/24C07C50/26C07C50/34
    • C07C46/00C07C37/07C07C39/42C07C45/513C07C45/62C07C45/63C07C45/66C07C46/06C07C49/697C07C50/32C07C2601/14C07C2601/16C07C2602/10C07F7/1852C07C49/747C07C50/24
    • Provided is a process of preparation of 2-[ trans ,-4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy- 1,4-naphthoquinone, i.e. Atovaquone [I] which is cost effective, green, and eco-friendly process, without separation of any diastereomers or geometric isomers of intermediates obtained during the reactions. Also provided is separation of ' cis ' and ' trans ' isomer of intermediates VI, VII and VIII through selective crystallization in an appropriate solvent. A method for converting 2-[ cis ,-4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone to 2-[ trans -4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-l,4-naphthoquinone in presence of Lewis/ Bronsted acid is also provided. A process for preparation of compound 2-(4-(4- chlorophenyl)- 1 -hydroxy cyclohexyl)-3,4-dihydronaphthalen- 1 (2H)-one [IV] comprising condensation of (1,2-dihydronaphthalen-4-yloxy)trimethylsilane [II] with 4-(4- chlorophenyl)cyclohexanone [III] in presence of Lewis acid in organic solvent. The invention also encompasses a highly efficient and atomeconomic process for synthesis of compound [III] i.e. 4-(4-chlorophenyl)cyclohexanone as well as a process for synthesis of 2-[ cis -4-(4'- chlorophenyl)cyclohexyl]-3-hydroxy-l,4-naphthoquinone. Further provided is a process for isomerization of cis- Atovaquone i.e. 2-[ cis -4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-l,4- naphthoquinone to tnms-Atovaquone i.e. 2-[ trans -4-(4'-chlorophenyl)cyclohexyl]-3- hydroxy- 1,4-naphthoquinone in presence of Lewis acid.
    • 提供制备2- [反式,4-(4'-氯苯基)环己基] -3-羟基-1,4-萘醌的方法,即具有成本效益,绿色和环保的Atovaquone [I] 方法,而不分离在反应期间获得的中间体的任何非对映异构体或几何异构体。 还提供了通过在合适的溶剂中选择性结晶来分离中间体VI,VII和VIII的“顺式”和“反式”异构体。 将2- [顺式,4-(4'-氯苯基)环己基] -3-羟基-1,4-萘醌转化为2- [反式-4-(4'-氯苯基)环己基] -3-羟基 还提供了路易斯/布朗斯台德酸存在下的1,4-萘醌。 制备化合物2-(4-(4-氯苯基)-1-羟基环己基)-3,4-二氢萘-1(2H) - 酮[Ⅳ]的方法,包括(1,2-二氢萘-4-基) 氧基)三甲基硅烷[II]与4-(4-氯苯基)环己酮[III]在路易斯酸存在下在有机溶剂中反应。 本发明还包括用于合成化合物[III]即4-(4-氯苯基)环己酮的高效和原子经济方法,以及合成2- [顺式-4-(4'-氯苯基)环己基] - 3-羟基-1,4-萘醌。 还提供了顺式 - 阿托瓦醌异构化方法,即2- [顺式-4-(4'-氯苯基)环己基] -3-羟基-1,4-萘醌与叔 - 阿托喹醌即2- [反式-4-( 4'-氯苯基)环己基] -3-羟基-1,4-萘醌在路易斯酸存在下进行。