A short, scalable synthesis towards cihunamide B (1) is reported. The feature of this report is the decagram-scale SNAr reaction of L-tryptophan derivatives followed by atroposelective Larock macrocyclization. This strategy allowed the scalable construction of a Trp-Trp cross-linkage with unprecedented atropisomerism. It has also enabled the scalable synthesis of cihunamide B (1), which is expected to be a potential antibacterial agent.
Experimental Procedures and Characterization of Compounds