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Direct remote C H functionalization in piperidine derivatives
The transition metal-catalyzed direct functionalization of C-H bonds is a major research topic across the world. However selective (regio-, enantio-, diastereoselective) and efficient functionalization of C(sp3)-H bonds, remains a... The transition metal-catalyzed direct functionalization of C-H bonds is a major research topic across the world. However selective (regio-, enantio-, diastereoselective) and efficient functionalization of C(sp3)-H bonds, remains a significant challenge: C(sp3)-H bonds are omnipresent in organic molecules and their dissociation energies are large. The use of directing groups (DGs) guiding the metal to specific C-H bonds and allowing intramolecular C-H bond activation, is a recognized general approach to address the selectivity challenge. However, their installation and removal add steps to the overall reaction sequence. This proposal aims to develop unprecedented regio- and diastereoselective transition metal-catalyzed functionalization of piperidine derivatives with haloalkenes making use of transient DGs, installed and removed in situ during catalysis. Access to a large number of substituted piperidines as well as known and new bicyclic scaffolds can be achieved via post-functionalization of the vinylpiperidine reaction products, making the aimed synthetic methodology potentially suitable for molecular library synthesis in drug discovery. A particularly challenging objective of the proposal is the remote (meta) functionalization with respect to the DG at C3 of the piperidine ring. Piperidine is chosen as a central heterocycle core in this application based on its importance in drug design and wide occurrence in commercial drugs (privileged scaffold). ver más
31/03/2021
UANTWERPEN
178K€
Duración del proyecto: 24 meses Fecha Inicio: 2019-03-26
Fecha Fin: 2021-03-31

Línea de financiación: concedida

El organismo H2020 notifico la concesión del proyecto el día 2021-03-31
Línea de financiación objetivo El proyecto se financió a través de la siguiente ayuda:
MSCA-IF-2018: Individual Fellowships
Cerrada hace 6 años
Presupuesto El presupuesto total del proyecto asciende a 178K€
Líder del proyecto
UNIVERSITEIT ANTWERPEN No se ha especificado una descripción o un objeto social para esta compañía.
Perfil tecnológico TRL 4-5