Author/Authors :
Houshdar Tehrani, Mohammad Hassan Department of Pharmaceutical Chemistry, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran , Farni, Morteza Department of Pharmaceutical Chemistry, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran , Shalchian Nazer, Massoud Department of Pharmaceutical Chemistry, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran
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
Keywords :
Baclofen , Synthesis , GABA receptor , Agonist
