Continuous flow synthesis of arylhydrazines <i>via</i> nickel/photoredox coupling of <i>tert</i>-butyl carbazate with aryl halides
作者:Alejandro Mata、Duc N. Tran、Ulrich Weigl、Jason D. Williams、C. Oliver Kappe
DOI:10.1039/d0cc06787c
日期:——
Nickel/photoredox catalyzed C–N couplings of hydrazine-derived nucleophiles provide a powerful alternative to Pd-catalyzed methods. This continuous-flowphotochemical protocol, optimized using design of experiments, achieves these couplings in short residence times, with high selectivity. A range of (hetero)aryl bromides and chlorides are compatible and understanding of process stability/reactor fouling
The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g.,
Pseudomonas aeruginosa
) and Gram-positive (e.g., methicillin-resistant
Staphylococcus aureus
) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.