Total Synthesis of Cyclotheonamide C using a Tandem Backbone-Extension-Coupling Methodology

摘要

The cyclotheonamides(Ct)are a family of nine macrocyclic pentapeptides isolated from the sponges Theonella swinhoei and ircinia.A common structural feature of these compounds is a highly electrophilic alpha-keto-beta-arginine(k-Arg)moiety,which is responsible for their potency as inhibitors of serine proteases of the trypsin family,including thrombin,for which IC_(50)values are in the 3-80 nM range.