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Late-stage borylation of complex molecules for the synthesis of proteolysis targeting chimeras (Protacs)

Lead Research Organisation: UNIVERSITY COLLEGE LONDON
Department Name: Chemistry

Abstract

This project will identify scope and limitation of existing C-H borylation methodologies against representative set of heterocycles.
- examine literature methods for the production and use of boron radicals and repeat literature methods to examine their applicability with unsymmetrical sp2-sp3 diboron species and develop a protocol for radical Minisci-type C-H borylation of heterocycles
- examine and optimise methods for converting born esters to linker.
- explore use of borylation toolbox for late-stage functionalisation of bioactive molecules
- synthesis of PROTACs using borylation methodology

Publications

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Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/N509577/1 30/09/2016 24/03/2022
1960804 Studentship EP/N509577/1 06/11/2017 04/05/2021 Matthew Cross