This review highlights the application of biopolymers of natural α-amino acids and its
derived wild-type peptides employed as organocatalysts for the asymmetric synthesis of various important
compounds published by researchers across the globe. The α-amino acid with L-configuration
is available commercially in the pure form and plays a crucial role in enantioselective chiral
molecule synthesis. Out of twenty natural amino acids, only one secondary amine-containing proline
amino acid exhibited revolution in the field of organocatalysis because of its rigid structure
and the formation of an imine like transition state during the reaction, which leads to more stereoselectivity.
Hence, it is referred to as a simple enzyme in organocatalyst. Chiral enantioselective organic
molecule synthesis has been further discussed by employing oligopeptides derived from the
natural amino acids as a robust biocatalyst that replaced enzyme catalysts. The di-, tri, tetra-,
penta- and oligopeptide derived from the natural amino acids are demonstrated as a potential
organocatalyst, whose catalytic activity and mechanistic pathways are reviewed in the present paper.
Several choices of organocatalyst are developed to achieve a facile and efficient stereoselective
synthesis of many complex natural products with optically pure isomer. Subsequently, the researcher
developed green and sustainable heterogeneous catalytic system containing organocatalyst
immobilized onto solid inorganic support or porous material for accelerating reaction rate with
asymmetric one isomer product through the heterogeneous phase. Further, researchers developed
heterogeneous organocatalysts-Metal-Organic Frameworks (MOFs) that emerged as alternative
simple and facile heterogeneous catalysts for the bulk production and flow reactor for enantioselective
synthesis. This review compiled many outstanding discoveries in organocatalysts derivative of
amino acids, peptides and heterogenized-MOFs employed for many organic transformations in research
and industrial applications.