Initially, we anticipated that the introduction of the biaryl moiety into the three amino acid residues could be achieved through modular C-H biarylation of L-Alanine. Subsequently, we planned the total synthesis of micitide 982 (1) through atroposelective Larock macrocyclization using Pd catalysts. Additionally, this modular synthesis approach was expected to allow the synthesis of micitide 982 (1) and analogs with various non-natural biaryl linkages.