Modular, Atroposelective Total Synthesis of Micitide 982

A modular, atroposelective total synthesis of micitide 982 (1) is reported. The feature of this report is the gram-scale C-H biarylation of N-phthaloyl-L-alanine followed by atroposelective Larock macrocyclization. This modular approach allowed the construction of a highly strained atrop-Tyr-Trp cross-linkage with unprecedented atropisomerism, as well as the first total synthesis of micitide 982 (1).