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Herein, we report a rhodium-catalyzed chemo-divergent reaction of oxetan-3-one and azetidin-3-ones with arylboronic acids. Ligand and temperature control selectively provide access to either tertiary alcohols (3-aryl oxetanols/azetidinols) via direct carbonyl addition or α-oxy/α-amino ketones via β-carbon elimination-initiated ring opening. This methodology bypasses stoichiometric organometallic reagents and specialized precursors, offering broad functional group tolerance and efficient access to carboxylic acid bioisosteres, while establishing a versatile catalytic platform for diversifying aliphatic small-ring systems in drug discovery.
Shen et al. (Wed,) studied this question.