DOI: 10.1039/d6qo01185c ISSN: 2052-4129
Reaction-manifold diversion enables general access to oxa-β-lactam chemical space
Kaoud Salama, Zeinab Saedi, Martina Kintlova, Tomas Ozdian, Fiorella Meneghetti, Matteo Mori, Marian Hajduch, Petr Dzubak, Jan Pokorný, Alexander DömlingDiverting the Ugi manifold with aminooxyacetic acid provides mild, general access to oxa-β-lactams. Structural analysis reveals pronounced nitrogen pyramidalization, enabling targeted cysteine covalent modification of NPM1 W288C.