Cover Feature: Highly Efficient Synthesis of a Staphylococcus aureus Targeting Payload to Enable the First Antibody–Antibiotic Conjugate (Chem. Eur. J. 12/2018). Issue 12 (8th January 2018)

• Record Type: Journal Article
• Authors: Linghu, Xin; Segraves, Nathaniel L.; Abramovich, Ifat; Wong, Nicholas; Müller, Barbara; Neubauer, Nadja; Fantasia, Serena; Rieth, Sebastian; Bachmann, Stephan; Jansen, Michael; Sowell, C. Gregory; Askin, David; Koenig, Stefan G.; Gosselin, Francis
• Is Part Of: Chemistry. Volume 24:Issue 12(2018)
• Page Start: 2792
• Page End: 2792
• Publication Date: 2018-01-08
• Subjects: antibiotics -- bacteria -- flow chemistry -- oxidation -- semi-continuous; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.201706013
• Languages: English
• ISSNs: 0947-6539

Abstract

Abstract : Targeting Staphylococcus aureus with innovation : As a sophisticated therapeutic construct, an antibody–antibiotic conjugate (AAC) requires a robust chemical process to furnish the linker–drug for conjugation. In our case, continuous flow processing allows for a sensitive oxidative condensation reaction to proceed via a recycle loop method. Further streamlined chemistry allows the deeply colored, quaternary ammonium salt linker–drug to be reproducibly accessed in good yield and purity. This challenging synthesis enables construction of the first AAC to help cut through the fog of antibiotic resistance. More information can be found in the Communication by S. G. Koenig et al. onpage 2837 .