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The synthesis of uracil/thymine containing tetra/trisubstituted imidazole derivatives was demonstrated using Ugi/Passerini-reaction followed by a postcyclization reaction sequence. The approach enables the one-pot facile construction of diverse compounds in moderate to excellent yields (47-82%). The 5-fluorouracil and 5-methyluracil moieties afford potentially bioactive molecules with drug-like properties. These scaffolds are currently being utilized in the screening deck of the European Lead Factory.

Original publication

DOI

10.1021/acscombsci.7b00145

Type

Journal article

Journal

ACS combinatorial science

Publication Date

04/2018

Volume

20

Pages

192 - 196

Addresses

University of Groningen , Department of Drug Design , A. Deusinglaan 1 , 9713 AV Groningen , The Netherlands.

Keywords

Humans, Imidazoles, Uracil, Thymine, Magnetic Resonance Spectroscopy, Molecular Structure, Cyclization, Hydrogen Bonding, Models, Molecular, Small Molecule Libraries