A gram-scale synthesis of a macrocyclic amidinourea with strong antifungal activity through a Fukuyama tri-protected polyamine intermediate

Systemic fungal infections are, nowadays, of crucial importance and, thus, in the last decade, we explored the great potential of natural and synthetic guanylated compounds, a great amount of work that led to the development of new non-azole antifungal compounds bearing a macrocycle, endowed with potent antifungal activity. We planned many biological assays to evaluate this class, implying always greater amount of compounds needed. This triggered us to setup a convenient strategy to prepare, in an easy and affordable way, grams of compound to be tested in excellent overall yield.