State Key Laboratory of Natural Medicines, Department of Medicinal Chemistry, China Pharmaceutical University, China.
Chem Commun (Camb). 2022 Feb 24;58(17):2850-2853. doi: 10.1039/d1cc07058d.
A copper-catalyzed enantioselective [3 + 3] cycloaddition of propargyl carbonates and pyrazolones has been disclosed. This reaction provided an efficient route to synthesize pyranopyrazoles containing a chiral quaternary carbon stereocenter in good yields with good to excellent enantioselectivities. In addition, the hydroxyl group in the products could be conveniently transformed into a variety of functional groups, such as aldehyde, nitrile, alkene, ester and amide groups, which further increased the synthetic value of this reaction.
一种铜催化的炔丙基碳酸酯和吡唑酮的对映选择性[3+3]环加成反应已经被揭示。该反应提供了一种有效的途径，以良好的产率和优异的对映选择性合成含有手性季碳中心的吡喃吡唑酮。此外，产物中的羟基可以方便地转化为各种官能团，如醛、腈、烯烃、酯和酰胺基团，这进一步增加了该反应的合成价值。
