Synthesis of Complex Phenols Enabled by a Rationally Designed Hydroxide Surrogate.
The conversion of aryl halides to phenols under mild reaction conditions is a longstanding and formidable challenge in organic chemistry. Herein, we report the rational design of a broadly applicable Pd-catalyzed method to prepare phenols with benzaldehyde oxime as a hydroxide surrogate. These reactions occur under mildly basic conditions and enable the late-stage hydroxylation of several functionally-dense drug-like aryl halides.
Department of Process Research and Development, Merck & Co., Inc., Rahway, NJ, USA.
Patrick S
0000-0002-6102-815X
PS
Fier
Department of Process Research and Development, Merck & Co., Inc., Rahway, NJ, USA.
Kevin M
KM
Maloney
cross-coupling; hydroxylation; medicinal chemistry; palladium; phenols