Department of Chemistry, Payame Noor University, PO BOX 19395-4697 Tehran, Iran.
γ-Aminobutiric acid (GABA), the major inhibitory neurotransmitter in the central nervous system is activated by the antispastic and muscle relaxant agent, Baclofen, which is a lipophilic derivative of GABA. Because of its biological and pharmacological importance, there are several reports in the literature about the synthesis of baclofen since 1962. In this study baclofen was easily synthesized by Claisen condensation of ethyl acetoacetate and p-chlorobenzaldehyde, formation of cyclic imide from β(p-chlorophenyl) glutaric acid and further Hoffmann rearrangement of β(p-chlorophenyl) glutarimid. Reagents used were inexpensive and commercially available. The overall yield of the reported strategy was 50% which is a good yield compare with other previous reports.