SYNTHESIS OF INTERMEDIATE OF ANTIBACTERIAL AGENT

摘要

PURPOSE:To prepare an acid addition salt of o-aminomethylphenylacetic acid, etc. useful as an acylation agent for the synthesis of an intermediate of an antibacterial agent, by the catalytic hydrogenation of o-cyanophenylacetic acid, etc. in a water-miscible inert solvent in the presence of a hydrogen halide. CONSTITUTION:The catalytic hydrogenation of the compound of formulaI(n is 1 or 2) in an inert solvent miscible with water (e.g. ethanol) in the presence of a hydrogen halide affords an acid addition salt of formula II (HX is hydrogen halide) useful for acylation. The acid addition salt is if necessary neutralized to obtain an acid of formula III for acylation. The compound of formula II or formula III can be converted to a novel active cephalosporin derivative of formula V useful as an antibacterial agent, a nutritive additive for animal feed, a remedy for the mastitis of livestock, etc., by protecting the amino group, coupling with the compound of formula IV, and removing the amino-protecting group.