Explore the words cloud of the LATE-STAGE project. It provides you a very rough idea of what is the project "LATE-STAGE" about.
The following table provides information about the project.
THE CHANCELLOR MASTERS AND SCHOLARSOF THE UNIVERSITY OF CAMBRIDGE
|Coordinator Country||United Kingdom [UK]|
|Total cost||183˙454 €|
|EC max contribution||183˙454 € (100%)|
1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
|Duration (year-month-day)||from 2016-03-01 to 2018-02-28|
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|1||THE CHANCELLOR MASTERS AND SCHOLARSOF THE UNIVERSITY OF CAMBRIDGE||UK (CAMBRIDGE)||coordinator||183˙454.00|
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.
|year||authors and title||journal||last update|
Jaime R. Cabrera-Pardo, Aaron Trowbridge, Manuel Nappi, Kyohei Ozaki, Matthew J. Gaunt
Selective Palladium(II)-Catalyzed Carbonylation of Methylene Î²-Câˆ’H Bonds in Aliphatic Amines
published pages: 11958-11962, ISSN: 1433-7851, DOI: 10.1002/anie.201706303
|Angewandte Chemie International Edition 56/39||2019-06-13|
Matthew James Gaunt, Manuel Nappi, Chuan He, William Whitehurst, Ben Chappell
Selective Reductive Elimination at Alkyl Pd(IV) via Dissociative Ligand Ionization Enables Catalytic C(sp3)-H Amination to Azetidines
published pages: , ISSN: 1433-7851, DOI: 10.1002/anie.201800519
|Angewandte Chemie International Edition||2019-06-13|
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