Synthesis Of Benzodiazepines Lactones

The Benzodiazepines are a psychotropic drugs class, which act in Central Nervous System (CNS) as positive allosteric modulator in GABA-A receptor, promoting the potentialization of the depressor effects of the neurotransmitter gamma-aminobutyric acid due to an increase of the chloride ions channel opening. The effect of this action results in biological properties such as anesthetics, antidepressants, anxiolytics, hypnotics and anticonvulsants. In view of these important properties, this work has how goal the synthesis of new benzodiazepine compounds, where the benzodiazepine nucleus it is fused with the butyrolactone ring (Scheme1). The reaction with Amberlite IR-120 promoving the formation of 5a-n derivatives with 60-93% of yield, and the catalyst manteining your efficiency after the reuse of 3 times. These compounds will be submitted a biologic assays, for to verify if they have action about the CNS and to determinate a potential application with studies of molecular Docking.