Abstract: The stereochemical configuration (i.e., the spatial arrangement of drug molecules and bioactive compounds are critically linked to their physiological activities, as different stereoisomers (such as enantiomers) frequently demonstrate substantially distinct pharmacological effects. Traditional asymmetric catalysis methods generally adhere to a “one key, one lock” paradigm, which only permits efficient synthesis of specific stereoisomers among numerous possibilities. However, medicinal chemistry research often requires comprehensive evaluation of all potential configurational isomers. The bimetallic synergistic catalysis strategy offers an effective solution to this challenge: by employing two distinct metal catalysts that function in a coordinated “hand-in-hand” manner to independently control the formation of different chiral centers, this approach enables the targeted synthesis of all stereoisomers through flexible combination of the two catalysts’ configurations. This article aims to introduce undergraduate students to fundamental knowledge of stereodivergent synthesis via bimetallic synergistic catalysis, using the asymmetric allylic substitution reaction as a case study to demonstrate how this cutting-edge field can be incorporated into undergraduate education to cultivate scientific thinking and stimulate innovative interest.

Key words: Asymmetric catalysis, Bimetallic synergistic catalysis, Metal catalysis, Stereodivergent synthesis, Undergraduate teaching