BoImAr: Borylation(Catalytic)-Imination-Arylation(Catalytic) - A New Synthetic ...

• Author(s): Mendes, Paulo J. ; Peixoto, Daniela ; S, Carolina ; Burke, Anthony J.
• Date: 2013
• Persistent ID: http://hdl.handle.net/10174/8854
• Origin: Repositório Científico da Universidade de Évora
• Subject(s): Borylation; Imination; Arylation; Catalytic; Degenerative deseases
• Document Type: Lecture
• Language: English

Description

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.