Z-4105 was prepared according to the reaction sequence as follows: The isoxazole intermediate (III) was obtained by one-pot 1,3-dipolar cycloaddition between acetonitrile oxide, in situ generated from chlorooxime (II), and propargyl alcohol. The oxidation of compound (III) with potassium permanganate gave the acid (IV), which was subsequently converted into the acid chloride (V) by Burdett's method. Finally, Z-4105 was synthesized from (V) and gamma-aminobutyric acid by means of Schotten-Baumann procedure.