Overcoming the Challenge of Meta-Methylation of Pyridine: A Cost-Effective Aldehyde-Catalyzed Strategy Brings New Breakthroughs

Overcoming the Challenge of Meta-Methylation of Pyridine: A Cost-Effective Aldehyde-Catalyzed Strategy Brings New Breakthroughs

Image source: J. Am. Chem. Soc.Introduction:The introduction of methyl groups can significantly enhance the activity of drugs, thus driving the development of various methylation strategies. Among these, C-H methylation is particularly noteworthy, but a universal method for meta-C-H methylation of pyridine—one of the most common nitrogen-containing heterocycles in pharmacophores—remains absent. This article reports a method … Read more

Stereodivergent Synthesis of Allylic All-Carbon Quaternary Centers by Bimetallic Iridium/Magnesium-Catalyzed Allylic Alkylation

Stereodivergent Synthesis of Allylic All-Carbon Quaternary Centers by Bimetallic Iridium/Magnesium-Catalyzed Allylic Alkylation

The research team led by Liu Yangbin from Peking University and Feng Xiaoming from Sichuan University optimized conditions using benzothiazole acetamide and trisubstituted allylic carbonates, successfully applying the “iridium/magnesium cooperative catalysis strategy” to the asymmetric allylic alkylation reaction of trisubstituted allylic electrophiles with non-cyclic nucleophiles (α-benzothiazole acetamide). Abstract The stereodivergent synthesis of structural motifs bearing … Read more