Base-Promoted Aminoamidation of Cinnamoyl Chlorides with Aryl Amines: Access to β-Amino Amides.

Herein, a base-promoted strategy for the synthesis of β-amino acids derivatives from α,β-unsaturated acyl chlorides derivatives and aryl amines has been described. In the presence of triethylamine, a tandem Michael addition and nucleophilic substitution progress was generated. The current method features readily available raw materials, mild reaction conditions, high atom economy, and wide tolerance for the coupling partners.

Palladium-catalyzed ligand-regulated divergent synthesis of pyrrole[2,3-]indoles and ureas from 2-ethynylanilines and isocyanides.

Herein, a palladium-catalyzed and ligand-controlled protocol for the divergent synthesis of pyrrole[2,3-]indole and urea derivatives has been described. Pyrrole[2,3-]indoles ("cyclization on" products) tandem cyclization of -alkynylanilines with isocyanides in the absence of a ligand and ureas ("cyclization off" products) oxidative amination of anilines with isocyanides in the presence of a ligand were obtained both in moderate to good yields with high selectivity. In this chemistry, cyclic and acyclic products were easily accessed with the same starting materials under the regulation of the ligand.

Rapid assembly of structurally diverse cyanamides and disulfanes base-mediated aminoalkylation of aryl thiourea.

A general method for the preparation of cyanamides and disulfanes from aryl thiourea and halide through a base-mediated strategy is described. Mercaptan and -aryl cyanamide are the key intermediates in the reaction. The current method is convenient, eco-friendly, and has high yields for the synthesis of substituted cyanamide and functional disulfanes in a one-pot procedure from readily available starting materials.