To produce the subject compound useful as a therapeutic agent for hyperlipemia in high a yield under milder conditions than those of a method without using a solvent by reacting a stoichiometrically excessive raw material with a stoichiometrically excessive K2CO3 in a two-layer system of water and an organic solvent according to a new method.

One mol N-(4-chlorobenzoyl)-tyramine represented by formula I is compounded with 1.7-2.3mol (preferably 3.0mol) ethyl α-bromoisobutyrate represented by formula II, 1.7-2.3mol K2CO3 and 0.1-1.3mol (preferably 1.0mol) phase-transfer catalyst, e.g. tetrabutylammonium bromide and reacted in a solvent prepared by compounding toluene with water at (8:2) to (4:6) mixing ratio at 60-100°C (preferably 80°C) for 3-24hr(preferably 3.5hr) to produce bezafibrate represented by formula III.