公开(公告)号：JPS6425767A

公开(公告)日：1989-01-27

申请号：JP7562388

申请日：1988-03-28

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： KAGARA KOUJI ,  GOSHIMA SHUNSUKE ,  TSUBOI HIROYUKI

IPC: C07F7/10 ,  C07D239/96

Abstract: PURPOSE:To easily and safely obtain the titled compound useful as a synthetic intermediate for anti-inflammatory agent or a synthetic intermediate for a drug for the remedy of complications of diabetes, in high yield at a low cost, by reacting a specific compound with a silylation agent and then a compound such as ethyl bromoacetate. CONSTITUTION:The objective compound of formula III can be produced by (1) reacting a compound of formula I (R is H or halogen) or its salt with a silylation agent [e.g. hexamethyldisilazane, trimethylchlorosilane or N,O-bis(trimethylsilyl)acetamide] in a solvent such as toluene usually under cooling or at room temperature, (2) reacting the product with a compound of formula II [R is alkyl, lower alkenyl, lower aralkyl or R -Z (R is carboxyl; Z is lower alkylene); X is acid residue] or its salt and, as necessary, (3) desilylating the reaction product. The desilylation is carried out by hydrolysis, alcoholysis, etc.