Macrocyclizations for
Medicinal Chemistry: Synthesis
of Druglike Macrocycles by High-Concentration Ullmann Coupling
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Abstract
Conditions have been identified for the efficient Ullmann
macrocyclization
of phenol and imidazole nucleophiles with aryl iodides at high reaction
concentrations of up to 100 mM and using 5–10 mol % loading
of an inexpensive copper catalyst. A range of substitution patterns
and ring sizes are tolerated, and the method has been exemplified
by the synthesis of a set of druglike macrocycles
