JPS6425767A - Production of quinazoline derivative or salt thereof - Google Patents

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<1> 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<2> is alkyl, lower alkenyl, lower aralkyl or R<3>-Z (R<3> 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.