The Journal of Organic Chemistry· 2026Q2
Modifications of Phenols with β-Lactam via Ring–Opening Reaction
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- Q2SCImago
- 2026year
Short summary
A new K2CO3-mediated method modifies phenols by opening β-lactam rings under mild conditions, yielding amino acid-introducing phenolic products in good to excellent yields.
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Key points
- A novel K2CO3-mediated reaction modifies phenols by opening β-lactam rings.
- The method yields amino acid-introducing phenolic products in good to excellent yields.
- It is compatible with diverse substituted phenols, phenol-containing drugs, and peptides.
- A preliminary conjugate of two drugs via a phenolic linker was successfully constructed.
AI-generated from the title and abstract; the full text is not read.
Abstract
Abstract We report a K2CO3-mediated modification of phenols via the ring-opening of β-lactams under mild conditions. This method is compatible with a broad range of substituted substrates, affording the corresponding amino acid-introducing phenolic products in good to excellent yields. The protocol is also successfully applied to the modification of various phenol-containing small-molecule drugs and peptides. Importantly, a preliminary attempt to employ β-lactam as a linkage for constructing conjugates between a phenolic drug and another drug was also achieved. The extremely mild reaction conditions make this work as a potential easily handled modification protocol for phenol drugs.
The authors' abstract, as published at the source. The Journal of Organic Chemistry, 2026 · DOI ↗
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Field: Organic Chemistry
Organic ChemistryChemistry