Amino acids as chiral building blocks

Abstract

This chapter is focused on the application of amino acids as building blocks in asymmetric synthesis. As a tool for accessing enantiopure compounds, amino acids have been used in four different ways, (i) as chiral precursors, (ii) as chiral reagents, (iii) as chiral auxiliaries, and (iv) as organocatalysts. For decades amino acids, particularly α-amino acids, have been used consistently for the synthesis of numerous target molecules, which are generally biologically active, and in the pharmaceutical and agrochemical sectors. Moreover, it was only in the last 40 years that they have come into their own, due to the development of the technologies mentioned above, and most particularly in the last 20 years in the case of organocatalysis – the field that won the Nobel prize in chemistry in 2021.