We kick off the post-Father’s-Day workweek with a new pre-print on ChemRxiv describing the application of our lab’s strategy for directed nucleopalladation of alkenes to the synthesis of carbo- and heterocycles via [3+2]-(hetero)annulation. Though the mechanistic details are rather different, this reaction takes inspiration from the venerable Larock indole synthesis, enabling access to diverse indolines, 2,3-dihydrobenzofurans, and indanes from readily available starting materials. Working in close collaboration with Pfizer’s Oncology Medicinal Chemistry team and the Liu group at the University of Pittsburgh, we were able to examine a broad swath of a heterocyclic structural space relevant to drug discovery and to flesh out the reaction mechanism. Congrats to this fantastic team of coworkers: Hui-Qi, Pranali, and Hou-Xiang from our lab; Joyann, Shouliang, Michelle and Indra from Pfizer; and Ilia and Peng from Pitt. Special shout-out to our two undergraduate co-authors Pranali and Hou-Xiang!

For a link to the pre-print, click here: https://chemrxiv.org/articles/Anti-Selective_3_2_Hetero_annulation_of_Non-Conjugated_Alkenes_via_Directed_Nucleopalladation/12510038