Research demonstrates efficient synthesis of aryl-substituted 4-hydroxycyclopent-2-enones using organocatalysis, highlighting its importance in chemistry.
Aryl-substituted 4-hydroxycyclopent-2-enones (AHCPs) are important scaffolds in a range of natural products and drug candidates, but catalytic asymmetric synthesis of AHCPs remains scarce. Here, we report the first organocatalyzed annulation between alkynyl 1,2-diketones and ynones, which affords a variety of AHCPs with good to excellent ee values. The reaction features a series of unique bond cleavage and formation processes, thus highlighting the significant value and irreplaceable role of 1,2-diketone in synthetic chemistry.
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Zhu et al. (2026) studied this question.
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