ABSTRACT
Compared with chemocatalysis, biocatalysis has some advantages, such as more efficiency, more environmentally benign, and better chemo, regio- and stereoselectivity. Optically active 1,2,3,4-tetrahydroquinolines (THQs) are particularly prominent in these areas, due to THQs being not only an important family of bioactive alkaloids widespread in natural products, but also valuable synthetic intermediates in organic chemistry, particularly for the preparation of pharmaceutical compounds; they are also employed as the starting materials for the preparation of novel chiral ligands. This chapter emphasizes the synthesis of chiral THQs catalyzed by biocatalyst. Many biocatalytic methods for preparing optically active THQs from substrates with substituents at C2 and C4 positions have been developed in the past several years, but low enantioselectivity was in part observed for substrates with bulky residues. Research in this field will concentrate in the future on how to develop efficient asymmetric methods toward substrates with sterically demanding residues at C3 position of THQs.
