Nankai team: Organoboron "knocks on" the "new door" of pyridine drug synthesis

Xinhua News Agency, Tianjin, March 28 (Zhang Jianxin, Wu Junhui) Pyridine compounds are one of the important basic raw materials for pesticides, pharmaceuticals, daily chemicals and other industries

Since its discovery in the 1840s, scientists have obtained many important achievements for the benefit of mankind through the modification of pyridine molecules, including the well-known pesticide and herbicide paraquat, anti-tumor drug nilotinib, and anti-tuberculosis drugs.

"By directly modifying the pyridine structure of drug molecules, new compounds with similar activities can be quickly obtained.

Electrophilic substitution reactions can also occur at the C3 position of pyridine, but only a few reactions such as halogenation and nitration are feasible, and the reaction conditions are very severe

Wang Xiaochen's group used the 1,4-dihydropyridine intermediate produced in the organoboron-catalyzed pyridine hydroboration reaction, and realized the C3 alkylation of pyridine by introducing an electrophile

"The new method provides a convenient, efficient, accurate and versatile new way for post-modification of pyridine-containing drug molecules

A few days ago, a paper introducing the work was published online in the international academic journal "Journal of the American Chemical Society"