First Synthesis and Anti‐Inflammatory Effects of Puerariafuran and its Derivatives

The total synthesis of puerariafuran and its derivatives was achieved for the first time by the direct reaction between substituted α‐bromoacetophenones and resorcinol. The reaction was mediated by neutral alumina and was fully regio‐controlled. Subsequently, the Sonogashira coupling method was applied for puerariafuran preparation. Finally, the anti‐inflammatory effects of these prepared compounds were evaluated in lipopolysaccharide ( LPS ) stimulated RAW 264.7 macrophages. The results revealed that puerariafuran and its derivatives show weak inhibition activity on the production of inflammatory‐mediated nitric oxide.