A General and Practical Synthesis of N-Aryl-3-[4-(imidazol-4-yl)-1,2,3-triazol-1-yl]benzamide Anti-Inflammatory Cytokine Inhibitors

A practical, safe, and efficient synthesis of anti‐inflammatory cytokine inhibitors was developed and implemented for a number of analogues. A key aspect of the process is an efficient, one‐pot, tandem copper‐catalyzed azidonation and Huisgen 1,3‐dipolar cycloaddition using silyl protected alkynes. Couple and click: A practical, safe, and efficient synthesis of N‐aryl‐3‐[4‐(imidazol‐4‐yl)‐1,2,3‐triazol‐1‐yl]benzamide anti‐inflammatory cytokine inhibitors was developed and implemented for a number of analogues. A key aspect of the process is an efficient, one‐pot, tandem copper‐catalyzed azidonation and Huisgen 1,3‐dipolar cycloaddition using silyl protected alkynes.