Università della Svizzera italiana

Isonitrile-based multicomponent synthesis of β-amino boronic acids as β-lactamase inhibitors

Bassini, Emanuele ; Gazzotti, Stefano ; Sannio, Filomena ; Lo Presti, Leonardo ; Sgrignani, Jacopo ; Docquier, Jean-Denis ; Grazioso, Giovanni ; Silvani, Alessandra

In: Antibiotics, 2020, vol. 9, no. 5, p. 21 p

The application of various isonitrile-based multicomponent reactions to protected (2-oxoethyl)boronic acid (as the carbonyl component) is described. The Ugi reaction, both in the four components and in the four centers–three components versions, and the van Leusen reaction, proved effective at providing small libraries of MIDA-protected β-aminoboronic acids. The corresponding free...