Metal-Free Boron-Mediated ortho-C–H Hydroxylation of N‑Benzyl-3,4,5-tribromopyrazoles

Organic Letters(2022)

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摘要
A novel route has been reported for C–H hydroxylation of benzyl compounds directed by a 3,4,5-tribromopyrazole auxiliary via boronation/oxidation using BBr3 and NaBO3·4H2O. The strategy exhibits outstanding site selectivity and affords the corresponding phenols in moderate to excellent yields under metal-free conditions. Besides, this protocol can be achieved in one pot, which is highly promising as a practical method for use in a multistep organic synthetic process.
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