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    • 2. 发明申请
    • Process for the preparation of 4-methyl-7-aminoquinolones
    • 制备4-甲基-7-氨基喹诺酮的方法
    • US20050222397A1
    • 2005-10-06
    • US10498456
    • 2002-12-03
    • Johannes BenkhoffBernd Lamatsch
    • Johannes BenkhoffBernd Lamatsch
    • C07B61/00C07C211/52C07C235/80C07D215/38C09B29/42C07D215/36
    • C07D215/38
    • The present invention relates to a process for the preparation of a compound of the general formula (1), which comprises converting a compound of the general formula (II), in an aprotic organic solvent in the presence of a catalytically active amount of a strong acid (catalyst) or of an agent that liberates a strong acid or of an ammonium salt of a strong acid, it also being possible for the catalyst to be part of the starting material/product, into a compound of formula I, wherein R5, R6 and R8 are each independently of the others a hydrogen atom, a nitro group, a sulfo group, a halogen atom, a pseudohalogen, a group COOR1 or CONHR2 or a C1-8 alkyl, C1-8 alkoxy or aryloxy radical, an amide group, a thioalkyl or thioaryl radical, an alkyl- or aryl-sulfonyl radical, an alkyl- or aryl-sulfinyl radical, a trifluoromethyl group or a phosphono group, R1 and R2 being a hydrogen atom or a C1-8 alkyl radical or an aryl or aralkyl radical, R10 is a group —C(O)CH2C(O)CH3 and R11 is a hydrogen atom or an acyl radical, or R10 and R11 are a group —C(O)CH2C(O)CH3. The process according to the invention is simple to perform and results in products of high chemical purity and high isomeric purity in a high yield.
    • 本发明涉及制备通式(1)化合物的方法,该方法包括在非质子传递的有机溶剂中,在催化活性量的强力存在下,将通式(II)的化合物 酸(催化剂)或释放强酸或强酸铵盐的试剂,也可以将催化剂作为原料/产物的一部分转化为式I化合物,其中R 1, 其中,R 6,R 6和R 8各自独立地为氢原子,硝基,磺基,卤原子, 假卤素,基团COOR 1或CONHR 2或C 1-8烷基,C 1-8烷氧基 或芳氧基,酰胺基,硫代烷基或硫代芳基,烷基 - 或芳基 - 磺酰基,烷基 - 或芳基 - 亚硫酰基,三氟甲基或膦酰基,R 1和 R 2是氢原子或C 1 1-8个烷基或芳基或芳烷基,R 10是基团-C(O)CH 2 C(O)CH 3和R 11是氢原子或酰基,或R 10和R 11是基团-C( O)CH 2 C(O)CH 3。 根据本发明的方法操作简单,产生高产率的高化学纯度和高异构纯度的产品。
    • 6. 发明授权
    • Process for the preparation of 4-methyl-7-aminoquinolones
    • 制备4-甲基-7-氨基喹诺酮的方法
    • US07144993B2
    • 2006-12-05
    • US10498456
    • 2002-12-03
    • Johannes BenkhoffBernd Lamatsch
    • Johannes BenkhoffBernd Lamatsch
    • C07D215/38C07C235/80
    • C07D215/38
    • The present invention relates to a process for the preparation of a compound of the general formula (I), which comprises converting a compound of the general formula (II), in an aprotic organic solvent in the presence of a catalytically active amount of a strong acid (catalyst) or of an agent that liberates a strong acid or of an ammonium salt of a strong acid, it also being possible for the catalyst to be part of the starting material/product, into a compound of formula I, wherein R5, R6 and R8 are each independently of the others a hydrogen atom, a nitro group, a sulfo group, a halogen atom, a pseudohalogen, a group COOR1 or CONHR2 or a C1-8 alkyl, C1-8 alkoxy or aryloxy radical, an amide group, a thioalkyl or thioaryl radical, an alkyl- or aryl-sulfonyl radical, an alkyl- or aryl-sulfinyl radical, a trifluoromethyl group or a phosphono group, R1 and R2 being a hydrogen atom or a C1-8 alkyl radical or an aryl or aralkyl radical, R10 is a group —C(O)CH2C(O)CH3 and R11 is a hydrogen atom or an acyl radical, or R10 and R11 are a group —C(O)CH2C(O)CH3. The process according to the invention is simple to perform and results in products of high chemical purity and high isomeric purity in a high yield
    • 本发明涉及一种制备通式(I)化合物的方法,该方法包括在非质子有机溶剂中,在催化活性量的强的存在下,将通式(II)的化合物 酸(催化剂)或释放强酸或强酸铵盐的试剂,也可以将催化剂作为原料/产物的一部分转化为式I化合物,其中R 1, 其中,R 6,R 6和R 8各自独立地为氢原子,硝基,磺基,卤原子, 假卤素,基团COOR 1或CONHR 2或C 1-8烷基,C 1-8烷氧基 或芳氧基,酰胺基,硫代烷基或硫代芳基,烷基 - 或芳基 - 磺酰基,烷基 - 或芳基 - 亚硫酰基,三氟甲基或膦酰基,R 1和 R 2是氢原子或C 1 1-8个烷基或芳基或芳烷基,R 10是基团-C(O)CH 2 C(O)CH 3和R 11是氢原子或酰基,或R 10和R 11是基团-C( O)CH 2 C(O)CH 3。 根据本发明的方法操作简单,产生高产率的高化学纯度和高异构纯度的产品