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    • 2. 发明授权
    • Process for the epimerization of aminated phthalideisoquinolines
    • 胺化苯酞异喹啉的差向异构化方法
    • US4704458A
    • 1987-11-03
    • US694160
    • 1985-01-23
    • Yoshiyuki TakedaOsamu KawashimaShiro FurukawaYasukazu Ogino
    • Yoshiyuki TakedaOsamu KawashimaShiro FurukawaYasukazu Ogino
    • C07D317/00C07D491/04C07D491/056C07D217/04C07D307/34
    • C07D491/04
    • Disclosed herein is an improved process for preparing 1RS-3'RS epimer of aminated phthalideisoquinolines represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen atom or a lower alkoxy group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen atom, amino group or a lower alkoxy group with at least one of R.sup.3 -R.sup.6 being amino group, and R.sup.7 is a lower alkyl group. The improvement comprises, after having reduced a mixture of epimers of corresponding nitro compounds of the general formula (I) wherein the amino group is replaced by nitro group into the amino compounds (I), treating said amino compound at a temperature in the range of 20.degree.-100.degree. C. in an aliphatic lower alcohol in the presence of an alkali to epimerize 1RS-3'SR epimer of said amino compound into said 1RS-3'RS epimer thereof.
    • 本文公开了一种用于制备由通式(I)表示的胺化苯并二氮杂异喹啉的1RS-3'RS差向异构体的改进方法:其中R 1和R 2独立地为氢原子或低级烷氧基,R 3,R 4, R 5和R 6独立地为氢原子,氨基或低级烷氧基,其中R 3 -R 6为氨基,R7为低级烷基。 改进之处在于将氨基被硝基替代为氨基化合物(I)的通式(I)的相应硝基化合物的差向异构体混合物在下列温度范围内处理: 20℃-100℃,在脂肪族低级醇中,在碱的存在下使所述氨基化合物的1RS-3'SR差向异构体差向异构化为所述1RS-3'RS差向异构体。