Amino acids are an important class of organic compounds wide applications in organic synthesis and medicinal chemistry. Most of natural amino acids are chiral compounds. Their activities are highly related with their stereochemistry. Development of new synthesis method of optically active amino acids is an important research top in organic chemistry.Enzymatic transamination is a very significant process in biological system, which provide various amino acids to maintain normal metabolism. Mimicking this biological process is not only of great importance to chemical biology, but also provides an attractive strategy to access chiral amino acids. We designed and synthesized a variety of BINOL-based chiral pyridoxals 6 and realized 6-catalyzed asymmetric transamination of α-keto acids under mild conditions to give various α-amino acids in good yields with low to moderate enantioselectivity. |