Achieving enantioselective construction of bridged-ring scaffolds presents a challenge, due to the considerable structural strain of the products and the presence of multiple stereocenters. Herein, the authors report a Pd/Cu co-catalyzed substrate-dependent enantiodivergent tandem Heck/Sonogashira reaction for synthesis of alkyne-tethered (R,S,S)-bicyclo[3.2.1]octenes and (S,R,R)-benzo-bicyclo[3.2.1]octanes, each featuring one quaternary and two adjacent tertiary stereocenters.
- Jing Zhong
- Mengxian Li
- Hequan Yao