Prof. Ying-Ming Pan and Hai-Tao Tang research group: nano-palladium catalyst for chemoselective synthesis of anti-tumor benzofuran [2,3-b]pyrazine

datetime: 2019-09-11 views: 61

We all know that ligands play a motor role in organic synthesis. If we can understand its electronic properties and spatial structure, we can design some ligands to coordinate with certain transition metals. Form a unique and novel transition metal catalyst system and use these catalyst systems to perfect or develop more organic synthesis reactions.

Metal/ligand homogeneous catalytic systems are widely used in many organic reactions, but their noble metal catalysts have high activity and poor selectivity, which limits their large-scale use in the reaction. In recent years, heterogeneous catalysis has been well used in hydrogenation, hydroformylation and other industrial synthetic applications due to its high catalytic activity, high selectivity and low cost, but it is intermediate between drug molecules and complex drugs. There are few applications in the synthesis of the body. In this context, we designed and synthesized a series of vinyl functionalized nitrogen and phosphorus ligand precursors, and then derived a series of nanocatalysts based on porous organic ligand polymers.

Recently, Professor Pan Yingming and Mr. Tang Haitao have developed a vinyl functionalized nano-polymer catalyst with a bidentate phosphorus ligand. This catalyst combines the advantages of homogeneous and heterogeneous catalysts and achieves high success. Regioselectivity and recyclability of more than 10 times. This method achieves the precise synthesis of a series of benzofuran [2,3-b]pyrazines. By screening in vitro for antitumor activity, we found that compound 3w has better antitumor activity. Further studies on anti-tumor mechanisms have shown that compound 3w can induce an increase in intracellular calcium and reactive oxygen species, inhibit T-24 tubulin polymerization, and cause cell apoptosis. Moreover, the method is more environmentally friendly than the conventional synthesis method.