N-Iodosuccinimide-Promoted Synthesis of Indolo[3,2-c]quinolizines via Cascade Intramolecular C–N Bond Formation/Aromatization with 3-(1H-Indol-3-yl)-2-(pyridin-2-yl)propanoates

The Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: April 10, 2025

An NIS-promoted cascade of intramolecular C-N bond formation/aromatization with 3-(1H-indol-3-yl)-2-(pyridin-2-yl)propanoates is described for synthesizing a polycyclic indole skeleton, indolo[3,2-c]quinolizine, as well 1,9-dihydropyrazolo[4',3':5,6]pyrido[2,3-b]indole. The advantages this protocol include accessible starting materials, mild conditions, simple operation, and good yields. Indolo[3,2-c]quinolizines exhibited fluorescence properties effective staining live cells, targeting lysosomes mitochondria. Additionally, the products showed significant antiproliferative activity against tumor cells in MTT assay.

Language: Английский

Photoinduced Decarboxylative Sulfonylation of Carboxylic Acids with Sodium Sulfinates

The Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: June 3, 2025

We report photoinduced decarboxylative sulfonylation of carboxylic acids with sodium sulfinates for synthesizing sulfones. The reaction proceeds under mild conditions, directly utilizing without prefunctionalization, copper acetate as the oxidant and base at room temperature. This method demonstrates excellent substrate compatibility, accommodating simple acids, drug molecules successfully converted into corresponding Furthermore, we developed a two-step, one-pot protocol that integrated two DABSO (DABCO-bis(sulfur dioxide) adduct) to synthesize Biological activity evaluation revealed molecule-derived sulfones exhibited antiproliferative against tumor cells.

Language: Английский