Over the recent decade tremendous interest has been developed on the synthetic modification of natural as well as non‐proteinogenic amino acids and non‐natural linkages due to their immensely important applications in proteomics, diagnosis, and drug delivery etc. They are synthetically important also. For example, due to the high natural abundance of enantiopure amino acids, they and their derivatives are regularly employed in the development of several interesting synthetic methods, total syntheses of biologically related structures as well as in ligand elaboration. Thus, the synthetic field possesses a direct impact on several basic and applied sciences. But up to date only limited numbers of reviews are available which either appeared almost half a decade earlier or covered very specific areas of this highly expanding topic. Many achievements have already been realized in this field in the meantime which urgently need to be documented. Therefore, to meet the need this review is intended to cover the emerging versatile synthetic methods on the modification of amino acids and related structures over the recent decade with the relevant details of their respective prospects and problems in the best possible systematic and concise manner. Wherever needed relevant mechanistic details are also described.