anti-Selective [3+2] (Hetero)annulation of Nonconjugated Alkenes via Directed Nucleopalladation
Joint efforts of the groups of McAlpine, Liu and Engle lead to useful 2,3-dihydrobenzofurans, indolines, and indanes.
Carbo- and heterocyclic core structures – such as 2,3-dihydro-benzofurans, indolines, and indanes – are common motifs in bioactive and therapeutic molecules, as well as in natural products. Due to their usefulness, it remains important to identify efficient routes to access these compounds easily, quickly, and inexpensively. The groups of Dr. Indrawan J. McAlpine from Pfizer Oncology Medicinal Chemistry (San Diego, USA), Professor Peng Liu from the University of Pittsburgh (USA) and Professor Keary M. Engle from the Scripps Research Institute (La Jolla, USA) collaborated on the work leading to the publication of the highlighted paper. In a joint effort the three research groups have discovered a method that provides direct access to useful 2,3-dihydrobenzofurans, indolines, and indanes by employing ambiphilic aryl halide coupling partners and non-conjugated alkenyl amides.