PREPARATION METHOD OF ACECLOFENAC AND ITS INTERMEDIATE

摘要

PURPOSE: An intermediate for preparing £2-(2,6-dichloroanilino)phenyl| acetoxyacetic acid (referred as "aceclofenac") used as an anti-inflammatory and analgesic agent, and methods for preparing aceclofenac are provided to improve production yield and purity without a process of waste heavy metal. CONSTITUTION: The intermediate which is used for preparing aceclofenac represented by the formula 1, is represented by the formula 2, wherein R1 and R2 are independent of each other and are an alkyl group of C1-C4. Aceclofenac is prepared by selectively hydrolyzing the intermediate of the formula 2 by using an acid in organic solvent. Preferably, the acid is HCl, H2SO4 or methanesulfonic acid; the solvent is alkyl acetate of C1-C5; and the reaction temperature is 20-40 deg.C. The intermediate of the formula 2 is prepared by reacting the alkali metal salt of compound of the formula 3 with the compound of the formula 4(X-CH2-COO-CH2OR¬1OR¬2) in solvent, wherein R1 and R2 are independent each other and are an alkyl group of C1-C4, and X is a halogen atom. Preferably X is Cl or Br; and the solvent is DMF or DMSO.