BoImAr: Borylation(Catalytic)-Imination-Arylation(Catalytic) - A New Synthetic Approach to Promising Alzheimer and Parkinson Drugs

Abstract

Although dramatic progress has been made in understanding the pathogenesis of neurodegenerative conditions of the aged population such as Alzheimer's disease, Parkinson's disease and Fronto-Temporal dementia, to date most of these diseases are incurable. Because of the aging population, these disorders pose a serious challenge to the health care system. Loss of synapses is probably the common neuropathological feature leading to dementia in these neurodegenerative disorders.1 Parkinson's disease is a progressive neurodegenerative condition caused by loss of dopamine producing cells in the substantia located in the basal ganglia causing motor, autonomic and cognitive impairments.2 Rasagiline is a potent, selective, irreversible inhibitor of monoamine oxidase (MAO) which is an anti-Parkinson drug.3 Herein, we present our innovative approach to the synthesis of several chiral amine4 -benzolactam analogues which involves a one-pot borylation-Imination-Arylation (BoImAr) sequence - the last step being a key intramolecular catalytic arylation reaction.