Synthesis of Amcenestrant (SAR439859): A Copper-Catalyzed Cross-Coupling Reaction as a Sustainable Alternative to Palladium-Catalyzed Suzuki Reaction

A cross-coupling reaction between an enol triflate and an aryl Grignard reagent using a copper catalyst, followed by a deprotection step, a Mitsunobu reaction, and a saponification, allowed for the synthesis of Amcenestrant (SAR439859). This approach, avoiding an expensive and toxic transition metal, is as efficient as the classical route but less expensive for accessing this selective estrogen-receptor degrader (SERD).