Development of a new Alternative approach for the synthesis of Baclofen

γ-Aminobutyric acid (GABA) is the most important inhibitory neurotransmitter in the central nervous system and plays an important role in coordinating local neural networks and the function of brain regions( ). GABA generally has three types of GABAA, GABAB, and GABA receptors in the brain. Baclofen is an aminobutyric acid (GABA) derivative that acts as a receptor agonist (GABA B) (۲ -۴ ). And has been introduced in ۱۹۷۰ to relieve spasms. GABAB receptors are activated by the antispastic and muscle relaxant agent, baclofen, which is the only selective and therapeutically useful GABAB agonist currently used(۵ ).Various ways have been presented for the synthesis of this drug Because of its biological and pharmacological importance(۶, ۷). For the first time in ۱۹۶۲, Heinrich Keberle Et al in Switzerland synthesized baclofen(۸). Presented several synthetic approaches that are highlighted in Scheme (۱).also in ۲۰۱۸, Ashutosh Jagtap et al an alternative route of synthesizing baclofen was patented(۹) Scheme (۲). This invention claims to be more cost-effective, environmentally friendly, and commercially scalable and baclofen has been synthesized with ۷۰ efficiency.Examining these articles, we found that in most of these methods, from Reducing agents such as (Pd/C) for converting compound (۷) to compound (۸) and from Reducing agent (H۲ /Ranye Ni) To convert compound (۱۴) To compound (۱) Used. Working with these reducing compounds has many problems, such as environmental pollution and its carcinogenic effects which may cause chemical burns if inhaled or if they come into contact with skin. Additionally, working with them on a large industrial scale(۱۰).

Keywords:

:baclofen , Synthesis , Hofmann rearrangement , GABA receptor