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Synthetic method converts propargyl amines to pyrrolinones using malonyl chloride, suggesting efficiency in drug synthesis.
Pyrrolinones are frequently found in biologically active natural products and pharmaceuticals. As such, their synthesis has been the focus of several methodological studies. Described herein is a synthetic method for the direct conversion of terminal or arylated propargyl amines to 3-pyrrolin-2-ones utilizing a malonyl chloride and an amine base at a low temperature. It is postulated that the key intermediate is an ammonium enolate generated during the initial premixing of the amine base and malonyl chloride.
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Nakhla et al. (2025) studied this question.
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