Journal
JOURNAL OF COMBINATORIAL CHEMISTRY
Volume 12, Issue 5, Pages 655-658Publisher
AMER CHEMICAL SOC
DOI: 10.1021/cc100098v
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Funding
- ICSN-CNRS (Gif-sur-Yvette, France)
- Fondation pour la Recherche Medicale
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The parallel synthesis of O-aryloxyamines remains an unfulfilled need in the field of medicinal chemistry and fragment-based approaches. To fill this gap a solution-phase two-step process based on (1) a copper-catalyzed cross-coupling of aryl boronic acids with a fluorous tagged N-hydroxyphthalimide, and (2) a supported aminolysis was designed and optimized using Taguchi's method. A library of O-aryloxyamines was synthesized in high yields with high purity and diversity.
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