公开(公告)号：KR1020000037954A

公开(公告)日：2000-07-05

申请号：KR1019980052783

申请日：1998-12-03

Applicant: 신풍제약주식회사

Inventor： 한신 ,  박우일 ,  이상민 ,  이재욱

IPC: C07C229/40

Abstract: PURPOSE: Provided is a process for producing a £2-(2,6-dichloroanilino)phenyl|acetoxy acetate (aceclofenac) being used for an antipyretic, an analgesic in a high purity and yield, which is an economical and safe process. CONSTITUTION: A aceclofenac (formula 1) is produced by hydrolyzing an ester of a 2,2,2-trihaloethyl ester £2-(2,6-dichloroanilino)phenyl|acetoxy acetate (formula 2) having two esters with Zn or Zn-Cu catalyst in a formic acid, an acetic acid or a trifluoro acetate at 30-60°C for 3-8 hrs. The compound (formula 2) is produced by reacting a sodium or potassium £2-(2,6-dichloroanilino)phenyl| acetate (diclofenac) and a trihaloethyl halo acetate in an equivalent ratio of 1:1.1-1.5 in a dimethyl formamide or a dimethyl sulfoxide at 30-50°C. In the formula, X is a halogen.

Abstract translation: 目的：提供一种用于解热的2-（2,6-二氯苯胺基）苯基|乙酰氧基乙酸酯（醋氯芬酸），高纯度和高产率的止痛剂的方法，这是一种经济且安全的方法。 组成：通过水解具有两个酯的2,2,2-三卤代乙基酯（2-（2,6-二氯苯胺基）苯基|乙酰氧基乙酸酯（式2））的酯来制备醋氯芬酸（式1），其具有Zn或Zn- Cu催化剂在甲酸，乙酸或三氟乙酸酯中在30-60℃下反应3-8小时。 化合物（式2）通过使2-或2,6-二（2,6-二氯苯胺基）苯基钠钠或钾反应来制备 乙酸酯（双氯芬酸）和三卤代乙酸卤乙酸酯，其当量比为1:1.1-1.5，在二甲基甲酰胺或二甲基亚砜中，在30-50℃。 在该式中，X是卤素。