The remaining challenges for the total synthesis of micitide 982 (1) are the introduction of side chain amino acid residues and the deprotection of protecting groups (Scheme 2). Compound 31, possessing the highly strained atrop-Tyr-Trp linkage obtained via Larock macrocyclization, was converted to 33 by removing the Boc and TES groups with HCl, followed by condensation with Boc-L-alanine (32) mediated by HATU. Subsequently, using the same method, each amino acid residue (Boc-L-glycine (10), Boc-L-alanine (32), Boc-L-leucine (9), Boc-L-alanine (32) was sequentially condensed, leading to the conversion to compound 37 with a long side chain. The resulting 37 was subjected to hydrolysis followed by introduction of L-histidine methyl ester (36) to give protected micitide 982 (38) in good yield (49% from 36) on a 1.6 g scale. The last remaining challenge for the total synthesis is deprotection. After removal of the Me-ether and Boc groups of protected micitide 982 (38) with BBr3, the total synthesis of micitide 982 (1) was achieved after hydrolysis of the Meester with LiOH.