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    Process for preparing 2-amino-5-cyanobenzoic acid derivatives
    2.
    发明授权
    Process for preparing 2-amino-5-cyanobenzoic acid derivatives 有权
    制备2-氨基-5-氰基苯甲酸衍生物的方法

    公开(公告)号：US08049029B2

    公开(公告)日：2011-11-01

    申请号：US12516807

    申请日：2007-12-18

    申请人： Joerg Bruening ,  Gary David Annis ,  Donald J Dumas ,  Rafael Shapiro

    发明人： Joerg Bruening ,  Gary David Annis ,  Donald J Dumas ,  Rafael Shapiro

    IPC分类号： C07C253/00

    CPC分类号： C07C253/14 ,  C07C231/12 ,  C07C233/65 ,  C07C255/58

    摘要： Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.

    摘要翻译： 公开了一种制备式1化合物的方法，包括使式2化合物与金属氰化物试剂，铜（I）盐试剂，碘化物盐试剂和至少一种式3化合物（其中R1是NHR3或OR4）接触 ; R2是CH3或Cl; R3是H，C1-C4烷基，环丙基，环丙基环丙基，环丙基甲基或甲基环丙基; R4是H或C1-C4烷基; Y为Br或Cl; X为NR 13或O; n为0或1; 并且R5，R6，R7，R8，R9，R10，R11，R12和R13如本公开所定义。 还公开了制备式2化合物的方法，其中Y是Br，R 1是NHR 3，包括将含溴的气体引入含有式4化合物的液体中，并且还公开了制备式5化合物的方法，其中 R14，R15，R16和Z如本公开中所定义，使用式1的化合物，其特征在于通过上述方法制备式1的化合物。

    PROCESS FOR PREPARING 2-AMINO-5-CYANOBENZOIC ACID DERIVATIVES
    7.
    发明申请
    PROCESS FOR PREPARING 2-AMINO-5-CYANOBENZOIC ACID DERIVATIVES 有权
    制备2-氨基-5-氰基苯甲酸衍生物的方法

    公开(公告)号：US20100063287A1

    公开(公告)日：2010-03-11

    申请号：US12596556

    申请日：2008-06-23

    申请人： Gary David Annis

    发明人： Gary David Annis

    IPC分类号： C07F15/04 ,  C07C233/65 ,  C07C255/63

    CPC分类号： C07D401/04 ,  C07C253/14 ,  C07D231/14 ,  C07F15/04 ,  C07C255/58

    摘要： Disclosed is a method for preparing a compound of Formula 1 comprising (1) contacting a compound of Formula 2, with (2) at least one alkali metal cyanide and (3) at least one compound of Formula 4 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; and X is Br, Cl or I.Also disclosed is a method for preparing a compound of Formula 4 comprising contacting a mixture of (i) at least one compound of Formula 9 and (ii) at least one metal reducing agent with (iii) dichlorobis(triphenylphosphine)nickel, and further disclosed is a method for removing nickel impurities from a mixture thereof with compounds of Formula 1 comprising contacting the mixture with oxygen in the presence of an aqueous cyanide solution, and additionally disclosed is a method for preparing a compound of Formula 5 wherein R5, R6, R7 and Z are as defined in the disclosure, using a compound of Formula 1, characterized by preparing the compound of Formula 1 by the method disclosed above.

    摘要翻译： 公开了制备式1化合物的方法，其包括（1）使式2的化合物与（2）至少一种碱金属氰化物和（3）至少一种式4的化合物（其中R 1是NHR 3或OR 4）接触; R2是CH3或Cl; R3是H，C1-C4烷基，环丙基，环丙基环丙基，环丙基甲基或甲基环丙基; R4是H或C1-C4烷基; 还公开了制备式4化合物的方法，包括使（i）至少一种式9化合物和（ii）至少一种金属还原剂与（iii）的混合物的混合物接触， 二氯双（三苯基膦）镍，并且还公开了一种从其与式I化合物的混合物中除去镍杂质的方法，包括在氰化水溶液存在下使该混合物与氧接触，另外公开了一种制备化合物的方法 其中R 5，R 6，R 7和Z如本公开所定义，使用式1的化合物，其特征在于通过上述方法制备式1的化合物。