tert-Butyl 4-Iodobutyrate is a versatile reactant used in the preparation of phosphorylated 3-heteroarylcoumarins that are employed in fluorescence microscopy and nanoscopy. It is also used in the preparation of α-Me α-carboxyalkyl amino acids that can be incorporated into phosphotyrosine-free peptides as Grb2 SH2-inhibitors and potential anticancer agents.