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    • 10. 发明授权
    • Process for preparing N-substituted 1H-pyrazole-5-carbonylchloride compounds
    • 制备N-取代的1H-吡唑-5-碳酰氯化合物的方法
    • US08921567B2
    • 2014-12-30
    • US14235556
    • 2012-08-10
    • Karsten KörberPrashant DeshmukhFlorian KaiserMichael RackTimo FrassettoGemma VeitchMarkus Kordes
    • Karsten KörberPrashant DeshmukhFlorian KaiserMichael RackTimo FrassettoGemma VeitchMarkus Kordes
    • C07D401/04
    • C07D401/04
    • The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group consisting of phosgene or a phosgene equivalent, to obtain a compound of formula (I).
    • 本发明涉及制备式(I)的N-取代的1H-吡唑-5-碳酰氯化合物的方法,其中R1是氢,卤素,氰基,C1-C6-烷基,C1-C6-氟烷基,C3 C 1-8 - 环烷基,C 3 -C 8 - 氟代环烷基,C 2 -C 6 - 烯基,C 2 -C 6 - 氟烯基,C 1 -C 6 - 烷氧基,C 1 -C 6 - 氟烷氧基,C 1 -C 4 - 氟烷氧基-C 1 -C 4烷基,苯基和 喜欢; 每个R 2独立地选自卤素,C 1 -C 6 - 烷基,C 1 -C 6 - 氟代烷基,C 3 -C 8 - 环烷基,C 3 -C 8 - 氟代环烷基,C 2 -C 6 - 烯基,C 2 -C 6 - 氟烯基,C 1 -C 6烷氧基, 苯基等; r为0,1,2,3或4; 包括以下步骤:i)将其中变量R1,R2和r各自如上定义的式(II)化合物与选自具有碳或氮键合的锂的锂基或与镁结合的碱的碱 具有碳结合镁的无机碱; 和ii)通过使步骤(i)中获得的产物与选自光气或光气当量的试剂反应来进行氯羰化反应,得到式(I)化合物。