Thiocillin I

Over the past half century, the absolute configuration of thiopeptide antibiotics such as Thiocillin I has baffled chemists until the first correct synthesis of Micrococcin P1 in 2009. At this point we had to answer two questions - first, does the absolute configuration hold true for its natural analogues? Second, can we design a more efficient synthesis of the tri-substituted pyridine core? The current synthesis sheds light on these problems especially for medicinal chemists who wish to explore the SAR for the purposes of drug development.