RESUMO
In comparison to iron(ii) halides, iron(ii) triflate exhibits a greater resistance towards reduction by p-tolylmagnesium bromide. This knowledge has led to the development of an iron(ii) triflate/N-heterocyclic carbene-catalysed cross-coupling system of aryl Grignard reagents with aryl chlorides and tosylates with high efficiency, even surpassing that of previously reported catalyst systems employing strongly coordinating counterions in some cases.
RESUMO
To develop novel neuroprotective agents, a library of novel arylalkenylpropargylamines was synthesized and tested for inhibitory activities against monoamine oxidases. From this, a number of highly potent and selective monoamine oxidase B inhibitors were identified. Selected compounds were also tested for neuroprotection in in vitro studies with PC-12 cells treated with 6-OHDA and rotenone, respectively. It was observed that some of the compounds tested yielded a marked increase in survival in PC-12 cells treated with the neurotoxins. This indicates that these propargylamines are able to confer protection against the effects of the toxins and may also be considered as novel disease-modifying anti-Parkinsonian agents, which are much needed for the therapy of Parkinson's disease.
Assuntos
Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/metabolismo , Fármacos Neuroprotetores/farmacologia , Pargilina/análogos & derivados , Doença de Parkinson/tratamento farmacológico , Propilaminas/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Humanos , Camundongos , Estrutura Molecular , Inibidores da Monoaminoxidase/síntese química , Inibidores da Monoaminoxidase/química , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Células PC12 , Pargilina/síntese química , Pargilina/química , Pargilina/farmacologia , Doença de Parkinson/enzimologia , Doença de Parkinson/metabolismo , Propilaminas/síntese química , Propilaminas/química , Ratos , Relação Estrutura-AtividadeRESUMO
A catalyst system comprising Fe2(O(t)Bu)6 and an N-heterocyclic carbene ligand enables efficient syntheses of (hetero)biaryls from the reactions of aryl Grignard reagents with a diverse spectrum of (hetero)aryl chlorides. Amongst the alkoxide and amide counterions investigated, tert-butoxide was the most effective in inhibiting the homocoupling of arylmagnesiums.
Assuntos
Compostos Férricos/química , Metano/análogos & derivados , Amidas/química , Catálise , Complexos de Coordenação/química , Compostos Heterocíclicos/química , Metano/química , Óxidos/químicaRESUMO
A synthetic method of azaspirocyclohexadienones has been developed through copper-catalyzed aerobic spirocyclization of biaryl-N-H-imines prepared by the reaction of biarylcarbonitriles and Grignard reagents.
