Metal-Free Catalyzed Oxidation/Decarboxylative [3+2] Cycloaddition Sequences of 3-Formylchromones to Access Pyrroles with Anti-Cancer Activity

An efficient and direct approach to pyrroles was successfully developed by employing 3-formylchromones as decarboxylative coupling partners, and facilitated by microwave irradiation. The protocol utilizes easily accessible feedstocks, a catalytic amount of DBU without any metals, resulting in high efficiency and regioselectivity. Notably, all synthesized products were evaluated against five different cancer cell lines and compound 3l selectively inhibited the proliferation of HCT116 cells with an IC50 value of 10.65 mu M.

Automated summary

A highly efficient and direct method for synthesizing pyrroles was successfully developed by using 3-formylchromones as decarboxylative coupling partners and facilitated by microwave irradiation. This approach utilizes easily accessible starting materials, a catalytic amount of DBU without any metal catalyst, resulting in high efficiency and regioselectivity. Notably, the synthesized compounds were evaluated against five different cancer cell lines, and compound 3l selectively inhibited the proliferation of HCT116 cells.