Peptide macrocycles have found applications that range from drug discovery to nanomaterials. These ring-shaped molecules have shown remarkable capacity for functional fine-tuning. Such capacity is enabled by the possibility of adjusting the peptide conformation using the techniques of chemical synthesis. Cyclic peptides have been difficult, and often impossible, to prepare using traditional synthetic methods. For macrocyclization to occur, the activated peptide must adopt an entropically disfavoured pre-cyclization conformation before forming the desired product. Here, we review recent solutions to some of the major challenges in this important area of contemporary synthesis.

in the Chemistry Department at USC in the tenure track. He was promoted to full professorship in 1994. Currently, he holds the Olah Nobel Laureate Chair in Hydrocarbon Chemistry with research contributions and interests in new fluorination methods, new synthetic methods, mechanistic studies of organic reactions, electrochemistry, and superacid and hydrocarbon chemistry. He has published more than 300 papers, book chapters, and review articles; coauthored 4 books; and holds 3 patents. He has received many honors and recognition. He is currently an Advisory Editor of the International Journal of Porphyrins and Pthalocyanins.

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The function of many biologically active molecules requires the presence of carbon-nitrogen bonds in strategic positions. The biosynthetic pathways leading to such bonds can be bypassed through chemical synthesis to synthesize natural products more efficiently and also to generate the molecular diversity unavailable in nature.

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