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Amine-Directed Diverse C(sp3)-H Functionalization

Objective

The development of new chemical transformations based on catalytic functionalization of unactivated C-H bonds has the potential to simplify the synthesis of complex molecules dramatically. Although some progress have been achieved in this emerging area, the selective transformation of aliphatic C-H bonds is still a challenge. This proposal aims to develop a new platform for the direct activation of unactivated sp3 C-H bonds of aliphatic amines and to apply this novel C(sp3)-H functionalization technology to synthesize diverse amine compounds. A key novel concept of this project is to use an unprotected aliphatic secondary amine as a native directing group, through a remarkable 4-membered-ring cyclometallation pathway. The goals of this proposal include: (I) developing unprecedented diverse C(sp3)-H functionalization of amine technology, accessing diverse functionalized amine compounds, (II) developing novel Pd-catalyzed enantioselective C-H functionalization methods to make enantioenriched chiral molecules, (III) application of this novel C(sp3)-H functionalization technology to make a library of diverse functionalized Salbutamol and Bupropion analogues, and screen them for biological and medicinal activities.

Fields of science (EuroSciVoc)

Programme(s)

Topic(s)

Funding Scheme

MSCA-IF-EF-ST - Standard EF

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Call for proposal

(opens in new window) H2020-MSCA-IF-2014

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Coordinator

THE CHANCELLOR MASTERS AND SCHOLARS OF THE UNIVERSITY OF CAMBRIDGE
Net EU contribution
€ 195 454,80
Address
TRINITY LANE THE OLD SCHOOLS
CB2 1TN CAMBRIDGE
United Kingdom
Region
East of England East Anglia Cambridgeshire CC
Activity type
Higher or Secondary Education Establishments
Links
Total cost
€ 195 454,80