<p>This review highlights recent developments in the base-catalyzed synthesis of β-aminophosphonates, an important class of organophosphorus compounds with broad relevance in synthetic and medicinal chemistry. Phosphorus-containing compounds play a critical role in drug discovery owing to their diverse biological activities and naturally occurring P-containing molecules often exhibit remarkable pharmacological properties. Among these, phosphonates have emerged as versatile intermediates in organic synthesis and are widely used as antibiotics, enzyme inhibitors, peptide mimetics, and diverse therapeutic agents. Their structural similarity to amino acids and phosphates enables them to act as stable bio-isosteres, making them particularly valuable as models of biologically active molecules. Therefore, the pursuit of efficient and broadly applicable synthetic strategies for phosphonates and related derivatives, especially those involving C–P bond formation, remains a central objective for synthetic chemists. In this context, base-promoted methodologies offer significant advantages, including mild reaction conditions, ease of operation, and improved yields. Sustained investigation and improvement of such protocols are therefore essential for expanding the accessibility of β-aminophosphonates and facilitating their applications across medicinal, biological, and materials chemistry.</p> Graphical abstract <p></p>

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Exploring various base-catalyzed approaches to the synthesis of β-aminophosphonates: a review

  • Rama Moorthy Appa,
  • Reddi Mohan Naidu Kalla,
  • Murali Sudileti,
  • Jaewoong Lee

摘要

This review highlights recent developments in the base-catalyzed synthesis of β-aminophosphonates, an important class of organophosphorus compounds with broad relevance in synthetic and medicinal chemistry. Phosphorus-containing compounds play a critical role in drug discovery owing to their diverse biological activities and naturally occurring P-containing molecules often exhibit remarkable pharmacological properties. Among these, phosphonates have emerged as versatile intermediates in organic synthesis and are widely used as antibiotics, enzyme inhibitors, peptide mimetics, and diverse therapeutic agents. Their structural similarity to amino acids and phosphates enables them to act as stable bio-isosteres, making them particularly valuable as models of biologically active molecules. Therefore, the pursuit of efficient and broadly applicable synthetic strategies for phosphonates and related derivatives, especially those involving C–P bond formation, remains a central objective for synthetic chemists. In this context, base-promoted methodologies offer significant advantages, including mild reaction conditions, ease of operation, and improved yields. Sustained investigation and improvement of such protocols are therefore essential for expanding the accessibility of β-aminophosphonates and facilitating their applications across medicinal, biological, and materials chemistry.

Graphical abstract