LATE-STAGE
Financiado
Palladium catalyzed C sp3 H late stage diversification of biologically active m...
Aliphatic amines are central to the function of many biologically active molecules as evidenced by their prevalence in a large number of pharmaceutical agents. The groups appended to these nitrogen atoms are crucial in determining...
Aliphatic amines are central to the function of many biologically active molecules as evidenced by their prevalence in a large number of pharmaceutical agents. The groups appended to these nitrogen atoms are crucial in determining the physical properties of the amine and are linked to how well it interacts with a biological target. Despite the apparent simplicity of the aliphatic amine motif, the number of general methods that allow their late-stage functionalization directly on the bioactive compound is surprisingly limited, and so the development of directed catalytic methods remains an important challenge. Metal catalysed C–H activation represents a versatile tool for late-stage functionalization. It mostly relies on directing functional groups to functionalize C–H bonds. Recently, Professor Gaunt at the University of Cambridge has uncovered a new C–H activation mode that enables the conversion of hindered amines into β-lactams and aziridines. The first objective of this proposal aims to directly apply the transformations developed by Gaunt, e.g. carbonylation, aziridination and acetoxylation reactions, to a precise class of drugs that contain the secondary amine motif as central function, i.e. β-adrenergic drugs. The use of the oxidative Pd(II)/(IV) catalytic cycle will then allow the development of a novel fluorination. The second objective relies on a new methodological concept, which seeks to merge palladium catalysis with radical chemistry, opening a route to develop novel perfluoroalkylation, amination and methylation reactions via a new Pd (II)/(III)/(IV) catalytic cycle. Finally, the third aim will be to apply all the methods developed to four important anticancer drugs, in collaboration with the new AstraZeneca oncology unit in Cambridge, to prepare novel analogues for biological testing.
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Duración del proyecto: 24 meses
Fecha Inicio: 2016-02-24
Fecha Fin: 2018-02-28
Fecha Fin: 2018-02-28
Línea de financiación: concedida
El organismo H2020 notifico la concesión del proyecto el día 2018-02-28
Línea de financiación objetivo
El proyecto se financió a través de la siguiente ayuda:
MSCA-IF-2015-EF:
Marie Skłodowska-Curie Individual Fellowships (IF-EF)
Cerrada
hace 9 años
Presupuesto
El presupuesto total del proyecto asciende a
183K€
Líder del proyecto
THE CHANCELLOR MASTERS AND SCHOLARS OF THE UN...
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Perfil tecnológico
TRL
4-5
Perfil tecnológico
TRL
4-5
258.89K€ |
Participante