Invention Grant
US08212075B2 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

Process for preparing 2-amino-5-cyanobenzoic acid derivatives
Abstract:
Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with at least one alkali metal cyanide of Formula 3 and a 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; X is Br, Cl or I; and R5, R6, R7, R8, R9 and R10 are as defined in the disclosure.Also disclosed is a method for preparing a compound of Formula 4 wherein R9 and R10 together are a cycloalkadiene bidentate ligand, comprising contacting a compound of Formula 5 wherein Y is Cl, Br or I, with a cycloalkadiene bidentate ligand, at least one metal reducing agent and a nitrile solvent.Also disclosed is a method for preparing a compound of Formula 1 comprising preparing a compound of Formula 4 by contacting a compound of Formula 5 with a cycloalkadiene bidentate ligand and at least one metal reducing agent, and then contacting the reaction mixture comprising the compound of Formula 4 with a compound of Formula 2 and at least one alkali metal cyanide of Formula 3; and further disclosed is a method for preparing a compound of Formula 6 wherein R15, R16, R17 and Z are as defined in the disclosure using a compound of Formula 1, characterized by preparing the compound of Formula 1 by a method disclosed above.
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