Ring fluorination of non-activated aromatic compounds
    122.
    发明授权
    Ring fluorination of non-activated aromatic compounds 失效
    非活化芳香族化合物的环氟化

    公开(公告)号:US06635760B2

    公开(公告)日:2003-10-21

    申请号:US10044082

    申请日:2001-10-23

    Abstract: Aromatic compounds having one or more electron-withdrawing substituents are fluorinated, preferably in a nitromethane solvent, by contact with tri(halo- or trifluoromethyl) substituted N-fluorotriazinium salts of the following Formula I: wherein three A moieties are independently CR, where each R is independently halogen or trifluoromethyl; two A moieties are independently Z, where each Z is independently nitrogen or a quaternary nitrogen atom and Y is a counterion or group of counterions which are inert to chemical attack by fluorine. Preferably the cation of the salt is 2,4,6-trichloro-1,3,5-triazinium.

    Abstract translation: 具有一个或多个吸电子取代基的芳族化合物优选通过与下式I的三(卤代或三氟甲基)取代的N-氟代三嗪鎓盐接触来氟化,优选在硝基甲烷溶剂中:其中三个A部分独立地为CR,其中每个 R独立地为卤素或三氟甲基; 两个A部分独立地为Z,其中每个Z独立地为氮或季氮原子,Y为对氟化学侵蚀呈惰性的抗衡离子的抗衡离子。 优选的盐的阳离子是2,4,6-三氯-1,3,5-三嗪鎓。

    Process for producing 5-fluorooxyindole and for producing intermediates therefor
    123.
    发明申请
    Process for producing 5-fluorooxyindole and for producing intermediates therefor 失效
    5-氟氧吲哚的制造方法及其中间体的制造方法

    公开(公告)号:US20030181731A1

    公开(公告)日:2003-09-25

    申请号:US10333316

    申请日:2003-01-16

    Abstract: The present invention discloses a process for preparing 5-fluorooxindole represented by the formula (3): 1 which comprises (A) a first step of cyclizing 2-(5-fluoro-2-nitrophenyl)malonic acid diester represented by the formula (1) : 2 wherein R1 and R2 may be the same or different from each other and each represents a group which does not participate in the reaction, under reductive conditions to form 5-fluorooxindole-3-carboxylic acid ester represented by the formula (2): 3 wherein R1 has he same meaning as defined above, and (B) then, a second step of decarboxylating the 5-fluorooxindole-3-carboxylic acid ester, and a process for preparing its synthetic intermediates.

    Abstract translation: 本发明公开了一种制备式(3)表示的5-氟羟吲哚的方法:其包括(A)使由式(1)表示的2-(5-氟-2-硝基苯基)丙二酸二酯环化的第一步骤, :其中R 1和R 2可以相同或不同,并且各自表示不参与反应的基团,在还原条件下形成5-氟羟吲哚-3-羧酸酯,由 式(2):其中R 1具有与上述相同的含义,(B)然后,使5-氟羟吲哚-3-羧酸酯脱羧的第二步骤及其合成中间体的制备方法。

    Process for preparing 2-chloro-4-nitroalkylbenzene
    127.
    发明授权
    Process for preparing 2-chloro-4-nitroalkylbenzene 失效
    2-氯-4-硝基烷基苯的制备方法

    公开(公告)号:US06255542B1

    公开(公告)日:2001-07-03

    申请号:US09643114

    申请日:2000-08-21

    CPC classification number: C07C201/12 C07C205/12

    Abstract: A process for preparing 2-chloro-4-nitroalkylbenzenes is provided which comprises a ring chlorination of 4-nitroalkylbenzenes with elemental chlorine or chlorine-releasing compounds in liquid phase and in the presence of Friedel-Crafts catalysts and specific sulphur-containing aromatic compounds as co-catalysts.

    Abstract translation: 提供了一种制备2-氯-4-硝基烷基苯的方法,其包括在液相中和在Friedel-Crafts催化剂和特定含硫芳族化合物存在下,将4-硝基烷基苯与元素氯或释放氯的化合物进行环氯化反应 助催化剂。

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