A Ketone Synthesisvia Cu(I)-Catalyzed RegioselectiveCoupling of 2‑Pyridylthioesters with Grignard Reagents: InQuest of Straightforward Access to Pharmaceuticals

For commercial production of SGLT2 inhibitors, cryogenic conditions (−78 °C) were required at the key <i>C</i>-glycosidation step, which has restricted their supply to the world market. To address the challenge, reported herein is a new synthetic method based on a new ketone synthesis by means of copper­(I)-catalyzed coupling of 2-pyridylthioesters with Grignard reagents. The facile transformation from the ketones to the final APIs was realized under mild conditions due to the use of readily cleavable acetyl protecting groups.