This work demonstrates the synthesis of substituted acids from α-ketoglutaric acid and Ugi reactions, suggesting efficiency in one-pot procedures.
A small library of bis- and tetraamides was synthesized by the Ugi reaction with α-ketoglutaric acid, tert -butyl isocyanide, aromatic aldehydes, and aromatic amines. When o -azidoanilines were used, azidated peptidomimetics were obtained, the post-cyclization of which by the aza-Wittig reaction yielded a series of substituted 3-(3-oxo-3,4-dihydroquinoxalin-2-yl)propanoic acids containing a pharmacophore quinoxalinone moiety. The tandem Ugi/aza-Wittig combination was also carried out in a one-pot procedure without isolation of the intermediate.
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Honcharov et al. (2025) studied this question.
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