This analysis demonstrates effective α-aminophosphonate synthesis, highlighting bioisosteres and potential in drug discovery.
In this study, we report a DNA-compatible synthetic approach for the construction of α-aminophosphonate derivatives─phosphorus-containing bioisosteres of α-amino acids─via the Kabachnik-Fields reaction. This multicomponent transformation proceeds under mild conditions, demonstrates a broad substrate scope, and exhibits excellent compatibility with subsequent enzymatic ligation. Its successful application to a mock library synthesis further underscores the potential of this method as a valuable addition to the toolbox of DEL-compatible chemistry.
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Choi et al. (2025) studied this question.
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