1‐(Acetylamino)thioxanthones and Derivatives: Synthesis From 1‐Halogenothioxanthones and Biological Properties

Several 1‐(acetylamino)thioxanthones and thiochromeno[4,3,2‐ de ]quinol‐2‐ones were synthesized to study some of their biological properties. Starting from 1‐chloro‐, 1‐bromo, and 1‐iodothioxanthones, either commercially available or prepared by deprotometalation, cross‐coupling reactions were optimized to deliver the 1‐(acetylamino)thioxanthones. Their cyclization was then performed to afford the expected thiochromeno[4,3,2‐ de ]quinol‐2‐ones. The formation of 1‐aminothioxanthones was also successfully achieved by coupling reaction with tert ‐butylcarbamate. The biological properties of representative compounds were finally evaluated, with promising results in the field of antibacterial and anti‐cancer activities.