Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 77, Issue 24, Pages 11079-11090Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo302089f
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- Pfizer Worldwide RD
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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.
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