Today we report a unique approach to heterocycle synthesis, in which a C(sp³)–H bond and a C(sp³)–X (X = N, O, or S) undergo catalytic coupling with an ambiphilic aryl halide under Pd(II)/Pd(IV) catalysis. The reaction leverages a C(sp³)–H activation/β-X elimination strategy for strong bond cleavage previously developed by our lab. The method can be used to prepare difficult-to-access non-proteinogenic amino acids from methionine and transfigure unstrained heterocyclic starting materials. Congrats to the entire project team: graduate student Hui-Qi, visiting undergrad Jing-Chen, and the fantastic group of collaborators from Pfizer!

Click here for a link to the paper in Angewandte Chemie, International Edition, click here: https://onlinelibrary.wiley.com/doi/10.1002/anie.202306581

As a reminder, a pre-print of this work was deposited in May 2023: https://chemrxiv.org/engage/chemrxiv/article-details/645c06c6f2112b41e956d61a