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Combined photochemical arylation, "nuisance effect" (S N Ar) reaction sequences have been employed in the design of small arrays for immediate deployment in medium throughput X-ray protein-ligand structure determination. Reactions have been deliberately let "out of control," in terms of selectivity; for example the ortho-arylation of 2-phenylpyridine gave five products resulting from mono-, bis- arylations combined with S N Ar processes.  As a result, a number of crystallographic hits against NUDT7, a key peroxisomal CoA ester hydrolase, have been identified.

Original publication

DOI

10.1002/cmdc.202000543

Type

Journal article

Journal

ChemMedChem

Publication Date

18/08/2020

Addresses

University of Sussex, School of Life Sciences, UNITED KINGDOM.