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Palladium catalyzed C(sp3)‒H late-stage diversification of biologically active molecules

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EC-Contrib. €

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Project "LATE-STAGE" data sheet

The following table provides information about the project.

Coordinator
THE CHANCELLOR MASTERS AND SCHOLARSOF THE UNIVERSITY OF CAMBRIDGE 

Organization address
address: TRINITY LANE THE OLD SCHOOLS
city: CAMBRIDGE
postcode: CB2 1TN
website: www.cam.ac.uk

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country United Kingdom [UK]
 Project website http://www-gaunt.ch.cam.ac.uk/publications.shtml
 Total cost 183˙454 €
 EC max contribution 183˙454 € (100%)
 Programme 1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
 Code Call H2020-MSCA-IF-2015
 Funding Scheme MSCA-IF-EF-ST
 Starting year 2016
 Duration (year-month-day) from 2016-03-01   to  2018-02-28

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    THE CHANCELLOR MASTERS AND SCHOLARSOF THE UNIVERSITY OF CAMBRIDGE UK (CAMBRIDGE) coordinator 183˙454.00

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 Project objective

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.

 Publications

year authors and title journal last update
List of publications.
2017 Jaime R. Cabrera-Pardo, Aaron Trowbridge, Manuel Nappi, Kyohei Ozaki, Matthew J. Gaunt
Selective Palladium(II)-Catalyzed Carbonylation of Methylene β-C−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
2018 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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