Fit‐for‐Purpose Synthesis of CDK2 Inhibitor GNE‐140

Abstract A six‐step, stereoselective synthesis of cyclin‐dependent kinase 2 (CDK2) inhibitor GNE‐140 was developed. The key bonds were assembled through palladium‐catalyzed Negishi cross‐coupling and Buchwald–Hartwig C−N coupling steps. The stereodiad was established through a single‐step, CuH‐catalyzed enone reduction proceeding in >99 : 1 er and 89 : 11 dr. GNE‐140 was obtained in 25 % overall yield with 98.6 A% HPLC purity.