A Novel Method for the Synthesis of Actarit

The specific synthetic route to synthesize the actarit (4-acetyl-amino phenylacetic acid) by acylation was designed in which p-amino benzaldehyde (a) and nitromethane (b) was used as the raw materials, through Knoevenagel reaction. The selective reduction of potassium borohydride and p-amino phenyl acetic acid to be oxidated under the acidic conditions. After optimization of the synthetic conditions, the I yield of each step was more than 85 %. The synthesized compound was confirmed by the elemental analysis and nuclear magnetic resonance. Because of the readily available raw materials, simple operations, high yield and avoiding highly toxic reagents in the synthesis of actarit (4-acetyl-amino phenylacetic acid), the synthetic route is suitable for the industrial production.