Herein a novel and concise approach to pyrrole skeletons via Pd-catalyzed tandem cyclization reactions is investigated. The substrates for the transformation could be readily prepared by phosphoric acid-catalyzed Ugi reactions with available starting materials. In this strategy, two isocyanides participate in sequential isocyanide insertion reactions, and the chemoselectivity of the products is regulated by the steric hindrance of the isocyanide. A plausible mechanism for the formation of the corresponding adducts is proposed.

In this work, an efficient synthesis of indole derivatives through palladium‐catalyzed double isocyanide insertion reactions has been developed. The reaction intermediates could be readily obtained by Ugi reactions. The transformation features broad functional‐group compatibility, commercially available starting materials, and moderate to good reaction yields. Furthermore, the bioactivities of the synthesized compounds were evaluated in mycelial growth tests against Penicilium digitatum and Colletotrichun gloeosporioides, and showed potential antifungal activities.

Herein, we report a novel one-pot method for synthesizing polysubstituted pyrrole derivatives via three-component reactions of alkenyl bromides, amines, and isocyanides. The conversion process is catalyzed by a Pd catalyst...

One-pot synthesis of azide-substituted dihydropyrazoles in isopropanol was performed using chalcones, hydrazine hydrate, and acyl chloride at 0℃, and its subsequent Staudinger-aza-Wittig-dehydroaromatization reactions with methyldiphenylphosphine were also investigated for further application in the construction of pyrazolo[1,5-c]quinazolines.