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Article Abstract
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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| http://dx.doi.org/10.1021/acs.orglett.5c03109 | DOI Listing |
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