Hefei National Laboratory for Physical Sciences at Microscale, CAS Key Laboratory of Soft Matter Chemistry, and Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, People's Republic of China.
Department of Chemistry and Chemical Engineering, Hefei Normal University, Hefei, Anhui 230601, People's Republic of China.
J Org Chem. 2021 Oct 15;86(20):14102-14112. doi: 10.1021/acs.joc.1c01472. Epub 2021 Aug 17.
The mechanochemical solvent-free synthesis of indenones from aromatic carboxylic acids and alkynes was achieved through triflic anhydride (TfO)-induced cyclization reaction. A variety of indenones including a bioactive PPARγ agonist were obtained in up to 90% yield at room temperature. The present protocol has the advantages of mild reaction conditions, high reaction efficiency, and feasibility of scalable synthesis, providing a facile and sustainable route to diverse indenones.
通过三氟甲磺酸酐（TfO）诱导的环化反应，实现了从芳香羧酸和炔烃到茚酮的机械化学无溶剂合成。在室温下，以高达 90%的产率获得了多种茚酮，包括一种具有生物活性的 PPARγ 激动剂。本方案具有反应条件温和、反应效率高、可规模化合成的特点，为各种茚酮的合成提供了一种简单、可持续的途径。
