Synthesis of Baclofen; an Alternative Approach

authors:

avatar Mohammad Hassan Houshdar Tehrani 1 , * , avatar Morteza Farnia 1 , avatar Massoud Shalchian Nazer 1

Department of Pharmaceutical Chemistry, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran, Iran

how to cite: Houshdar Tehrani M H, Farnia M, Shalchian Nazer M. Synthesis of Baclofen; an Alternative Approach. Iran J Pharm Res. 2003;2(1):e127600. https://doi.org/10.22037/ijpr.2010.26.

Abstract

γ -Aminobutiric acid (GABA), the major inhibitory neurotransmitter in the central nervous system has two major receptor subtypes (GABAA and GABAB). GABAB receptors are activated by the antispastic and muscle relaxant agent, Baclofen, which is a lipophilic derivative of GABA. Since 1962 several strategies have been reported for the synthesis of baclofen.In this study an approach has been made to synthesize baclofen in an alternative way. The key steps involved the condensation of p-chloro benzaldehyde with nitromethane and the reaction of β-nitro styrene thus prepared with malonate diethyl ester. Further reduction and decarboxylation of the product gave access to baclofen with a good yield.