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    • 10. 发明授权
    • Process for preparing 1-phenylpyrazoles
    • 1-苯基吡唑的制备方法
    • US08362271B2
    • 2013-01-29
    • US13393624
    • 2010-09-03
    • Maximilian DochnahlGunter Lipowsky
    • Maximilian DochnahlGunter Lipowsky
    • C07D231/10
    • C07D231/20C07D231/14
    • The present invention to a process for preparing 1-phenylpyrazoles of the formula I in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with apyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.
    • 本发明涉及一种制备式I的1-苯基吡唑的方法,其中每个R 1独立地选自氯,氟,烷基,卤代烷基,烷氧基和卤代烷氧基; n为1,2或3; 每个R 2独立地选自氰基,硝基,卤素,烷基,卤代烷基,烷氧基,卤代烷氧基,烷硫基和烷氧基羰基; m为0,1或2; A是烷基,芳基或芳基-C 1 -C 4 - 烷基,其中A任选地带有1,2,3或4个取代基,包括使式(II)的苯基卤与式(III)的吡咯衍生物反应,其中X为 氯,碘或溴; 在碱和催化体系的存在下,R 1,n,R 2,m和A各自如上所定义,所述催化体系包含配体和选自钯化合物,铁化合物和铜化合物的金属化合物。