Process for the preparation of substituted phenylacetic acid derivates and intermediates.

摘要

The prepn. of phenyl ethanoic acid derivs. of formula (I) comprises reacting sulphonyloxy activated hydroxyethanoic acid derivs. of formula (II) with aromatic cpds. of formula (III) opt. in the presence of a diluent and in the presence of an acid and then opt. hydrolysing. R3SO2OCH2R1 + Ar-H ArCH2R1 (II) (III) (I) Ar = Ph opt. mono to penta substd. with halogen, alkyl, alkoxy, haloalkyl, haloalkoxy, alkyl-carbonylamino opt. substd. aryl and/or opt. substd. aryloxy; R1 = CN, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or COOR2; R2 = H, opt. substd. alkyl, alkenyl, haloalkyl, opt. substd. aryl or opt. substd. aralkyl; R3 = halogen, alkyl, haloalkyl, opt. substd. aryl or opt. substd. benzyl. Also claimed are sulphonylated glycolic acid n-butyl esters of formula (IIa) (excepting the cpd. ethanoic acid ((fluorosulphonyl)oxy)n-butyl ester), and phenyl-ethanoic acid esters of formula (Ia): R3SO2OCH2 (IIa) Ar1CH2COOC4H9n (Ia) Ar1 = Ph which is tri substd. with opt. different 1-6C alkyl gps.