A facile and efficient synthesis of Baclofen

γ-Aminobutiric acid (GABA), the major inhibitory neurotransmitter in the central nervoussystem, is activated by the antispastic and muscle relaxant agent, Baclofen, which is a lipophilicderivative of GABA. Since 1962 several strategies have been reported for the synthesis ofbaclofen. In this study, baclofen was easily synthesized by Claisen condensation of ethylacetoacetate and p-chlorobenzaldehyde, which is formation of cyclic imide from β(pchlorophenyl)glutaric acid and further Hoffmann rearrangement of β(p-chlorophenyl) glutarimidwith a good yield.

Keywords:

Baclofen , synthesis , GABA receptor , γ-aminobutiric acid