Biocatalytic Construction of Two or More Stereocenters in the Synthesis of High-Value-Added Chemicals

Molecules containing multiple chiral centers can exist as various stereoisomers, each exhibiting distinct biological activities and pharmacological effects due to differences in spatial configuration. These variations may influence both the efficacy and the safety of the corresponding compounds. Consequently, great efforts have been devoted to developing efficient methods for the selective production of single stereoisomers of target molecules. Owing to their unparalleled stereoselectivity, biocatalytic approaches have significantly advanced the construction of chiral centers in complex molecules. In recent years, substrate-based, enzyme-based, and cascade reaction strategies have been intensively explored for the synthesis of molecules bearing multiple stereocenters. In this Perspective, we summarize recent advances in these strategies and highlight their complementary roles in the synthesis of bioactive compounds with multiple stereocenters, which will further promote the development of the fine chemical and pharmaceutical industries.