由亚磺酸酯和2-硼基苯胺合成噻吩并菲啶酮

Nakamura Keisuke, Suzuki Minori, Yoshida Suguru

Department of Biological Science and Technology, Faculty of Advanced Engineering, Tokyo University of Science, 6-3-1 Niijuku, Katsushika-ku, Tokyo 125-8585, Japan.

Org Lett. 2024 Nov 15;26(45):9676-9681. doi: 10.1021/acs.orglett.4c03420. Epub 2024 Nov 6.

A facile palladium-catalyzed synthesis of thiaphenanthridinones from sulfinate esters and 2-borylanilines is disclosed. Various sulfur analogs of phenanthridinones were synthesized by bromide-selective cross-coupling and cyclization in one step. Further transformations of the obtained thiaphenanthridinones allowed preparing a broad range of thiaphenanthridinone derivatives involving analogs of bioactive compounds.

公开了一种由亚磺酸酯和2-硼基苯胺通过钯催化简便合成硫代菲啶酮的方法。通过一步溴化物选择性交叉偶联和环化反应合成了菲啶酮的各种硫类似物。所得硫代菲啶酮的进一步转化使得能够制备一系列广泛的硫代菲啶酮衍生物，包括生物活性化合物的类似物。