Pure 2-heterocyclylmethyl-benzoic acid derivative preparation in high yield, for use as pharmaceutical or agrochemical intermediate, from phthalide compound and nitrogen-containing heterocycle

摘要

Preparation of 2-((N-bonded heterocyclyl)-methyl)-benzoic acid derivatives (I) involves reacting a phthalide (II) with a nitrogen-containing heterocycle (III) (or its metal salt) in presence of a polar aprotic diluent and a optionally a basic reaction auxiliary. Preparation of 2-heterocyclylmethyl-benzoic acid derivatives of formula (I) involves reacting a phthalide of formula (II) with a nitrogen-containing heterocycle of formula H-Y (III) (or its metal salt) in presence of a polar aprotic diluent and a optionally a basic reaction auxiliary. n = 0-3; X = NO2, CN, CONH2, CSNH2, halo or (all optionally substituted) alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl; Y = N-bonded heterocyclyl.