Patent ID: 6426420
Filing Date: 2002-07-30
Classification: C07C,C07D,Y02P

Abstract:
A process for producing an isocoumarin-3-yl-acetic acid derivative represented by the following formula (I): (wherein R represents a hydrogen atom, a non-substituted or substituted alkyl group, a non-substituted or substituted alkenyl group, a non-substituted or substituted alkynyl group, a non-substituted or substituted alkoxyl group, a protected amino group, a hydroxyl group or a protected hydroxyl group; Ra represents a hydrogen atom or a protecting group for a carboxyl group; Rb represents a hydrogen atom or a protecting group for a hydroxyl group; and Rc represents a non-substituted or substituted lower alkyl group),said process comprising:reacting a homophthalic acid derivative represented by the following formula (III): (wherein Rc represents a nonsubstituted or substituted alkyl group; R1 represents a hydrogen atom or a protecting group for a carboxyl group; and R2 represents a hydrogen atom or a protecting group for a hydroxyl group) with a malonic acid derivative represented by the following formula (IV): (wherein R is as defined for formula (I); R3 represents a protecting group for a carboxyl group; and X represents a â€”OM group (wherein M is alkaline metal or alkaline earth metal), chlorine or bromine) in an inert organic solvent in the presence of a condensing agent, wherein a &bgr;-oxocarboxylic acid derivative represented by the following formula (II) in optionally formed during the above reaction: (wherein R and Rc are as defined for formula (I), and R1, R2 and R3 are as defined for formulas (III) and (IV)); and the protecting groups for the hydroxyl group and/or the carboxyl group are subjected to an elimination reaction, if necessary.