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A Novel Synthesis of Disubstituted Quinazoline Diones with Differential N-Substitution via a Copper-Catalysed Cross-Coupling of Acyl Ureas

Emma Durham, Dave Perkins*, James S. Scott, Jimmy Wang, Sam Watson

*AstraZeneca Pharmaceuticals, Alderley Park, Macclesfield, SK10 4TG, UK, Email:

E. Durham, D. Perkins, J. S. Scott, J. Wang, S. Watson, Synlett, 2016, 27, 965-968.

DOI: 10.1055/s-0035-1561500

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An efficient method for the synthesis of disubstituted quinazoline diones with differential N-substitution proceeds in high yields under mild conditions. The reaction tolerates a wide range of substitutions on the aromatic and dione rings.

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Key Words

acyl ureas, quinazoline diones, quinazolinediones, copper-catalysed, Ullmann reaction, intramolecular cyclisation

ID: J60-Y2016