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    • 9. 发明申请
    • Process for Manufacturing Substituted 5-Methoxymethylpyridine-2,3-Dicarboxylic Acid Derivatives
    • 制备取代的5-甲氧基甲基吡啶-2,3-二羧酸衍生物的方法
    • US20110245506A1
    • 2011-10-06
    • US13133008
    • 2009-12-07
    • David Cortes
    • David Cortes
    • C07D213/803C07D213/84C07D401/04
    • C07D213/84C07D213/80C07D401/04
    • A process for manufacturing a 2,3-disubstituted-5-methoxymethylpyridine of formula (I), where Z is H or halogen; Z1 is H, halogen, CN or NO2; Y2 is OM, and M is an alkali metal or an alkaline earth metal, comprises the step of: (i) reacting a compound of formula (II) where Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is H or halogen; Z1 is H, halogen, CN or NO2; Y1 and Y2 are each independently OR1, NR1R2, or when taken together Y1Y2 is —O—, —S— or —NR3—; R1 and R2 are each independently H, C1-C4 alkyl optionally substituted with C1-C1 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is H or C1-C4 alkyl, in a methanol/H2O mixture, comprising at least 20% by weight H2O (based on the sum of water and bromide (II)), with a base comprising MOCH3 and/or MOH, where M is alkali metal or alkaline earth metal, under pressure in a closed vessel at a temperature of from 75 to 110° C. Compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.
    • 制备式(I)的2,3-二取代-5-甲氧基甲基吡啶的方法,其中Z是H或卤素; Z1是H,卤素,CN或NO2; Y2是OM,M是碱金属或碱土金属,包括以下步骤:(i)使Q为叔脂族或环状饱和,部分不饱和或芳族胺的式(II)化合物反应; Z是H或卤素; Z1是H,卤素,CN或NO2; Y1和Y2各自独立地为OR1,NR1R2,或者当Y1Y2为-O - , - S-或-NR3-时; R 1和R 2各自独立地为H,任选地被C 1 -C 1烷氧基取代的C 1 -C 4烷基或任选被一至三个C 1 -C 4烷基,C 1 -C 4烷氧基或卤素原子取代的苯基,或任选被一至三个 C1-C4烷基,C1-C4烷氧基或卤原子; 在甲醇/ H 2 O混合物中,R 3是H或C 1 -C 4烷基,其包含至少20重量%的H 2 O(基于水和溴(II)的总和))与包含MOCH 3和/或MOH的碱,其中M 是碱金属或碱土金属,在密封容器中在75〜110℃的温度下进行加压。式(I)化合物是合成除草咪唑啉酮类似咪唑氧化物的有用中间体。