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
    • 3. 发明申请
    • NEW PROCESS FOR THE PREPARATION OF SPIRO [(4-CYCLOHEXANONE)-[3H]INDOL]-2'[1'<i>H</i>]-ONE DERIVATIVES
    • 制备螺[(4-环己酮) - [3H]吲哚] -2'[1'H] - 一种衍生物的新方法
    • WO0105760A2
    • 2001-01-25
    • PCT/HU0000081
    • 2000-07-13
    • SANOFI SYNTHELABOGOENCZI CSABACSIKOS EVAHERMECZ ISTVANHEJA GERGELYILLAR ARPADNAGY LAJOSSANTANE CSUTOR ANDREASIMON ATTILASIMON KALMANSMELKONE ESEK AGOTASZOMOR TIBORNESZVOBODA GYOERGYNE
    • GOENCZI CSABACSIKOS EVAHERMECZ ISTVANHEJA GERGELYILLAR ARPADNAGY LAJOSSANTANE CSUTOR ANDREASIMON ATTILASIMON KALMANSMELKONE ESEK AGOTASZOMOR TIBORNESZVOBODA GYOERGYNE
    • C07B61/00C07D209/34C07D209/96C07D405/04C07D209/00
    • C07D405/04C07D209/34C07D209/96Y02P20/55
    • The invention relates to a process for the preparation of spiro[(4-cyclohexanone)- [3H]indol]- 2'[1'H]- one derivatives of general formula (I) - wherein R and R independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4 polyfluoroalkyl, C1-4 polyfluoroalkoxy, C3-7 cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group -, characterized by reacting an indolin-2-one derivative of general formula (II) - wherein R and R are as defined above - with a compound capable for introducing a protective group, coupling the compound of general formula (III), thus obtained - wherein R and R are as defined above and A stands for a protective group - with acrylic acid C1-4ester, cyclizing the resulting compound of general formula (IV)- wherein R and R are as defined above - with a compound capable for introducing a protective group, coupling the compound of formula (III) thus obtained, - wherein R and R are as defined above and A stands for a protective group - with an acrylic acid C ester; cyclizing the resulting compound of formula (IV) - wherein R and R are as defined above R stands for C1-4alkyl and A stands for a protective group -, eliminating the -COOR group and the A protective group of the keto-ester of general formula (V) - wherein R and R are as defined above, R stands for C1-4alkyl and A stands for a protective group -, optionally without isolation of the compounds of general formulae (IV) and/or (V) and/or (VI).
    • 本发明涉及制备通式(I)的螺[(4-环己酮) - [3H]吲哚] -2'[1'H] - 酮衍生物的方法,其中R 1和R 2 独立地表示氢,C1-4烷基,C1-4烷氧基,C1-4烷硫基,C1-4多氟烷基,C1-4多氟烷氧基,C3-7环烷氧基,C3-7环烷硫基,苯氧基,苄氧基或硝基 - (II)(其中R 1和R 2如上定义)与能够引入保护基的化合物反应,将由此获得的通式(III)的化合物与通式 其中R 1和R 2定义如上,A代表保护基 - 与丙烯酸C 1-4酯反应,环化得到的通式(IV)的化合物 - 其中R 1和R 2如式 如上所定义的 - 与能够引入保护基团的化合物偶联,由此获得的式(III)化合物,其中R 1和R 2如上所定义,A代表 保护基 - 用丙烯酸C 1-4酯; 环化得到的式(IV)化合物 - 其中R 1和R 2如上所定义,R 3代表C 1-4烷基,A代表保护基 - 除去-COOR 3基团 和通式(V)的酮基的A保护基 - 其中R 1和R 2如上所定义,R 3代表C 1-4烷基,A代表保护基 - , - 任选不分离通式(IV)和/或(V)和/或(VI)的化合物。