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

Matteo Borgini, Francesco Orofino, Giuseppina I. Truglio, Lorenzo Balestri, Maurizio Botta, Janine Cossy
2019 ARKIVOC  
Dedicated to Steve, thanking him for his great ability to teach and his dedication Abstract 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
more » ... 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.
doi:10.24820/ark.5550190.p010.895 fatcat:kjvnr4r2rbe7lexe3b33ch6ue4