A series of peptide-based transition-state human neutrophil elastase (HNE) inhibitors with N-terminal acidic moieties were synthesized and their inhibitory activity against HNE was evaluated both in vitro and in vivo. Our results show that compounds containing cyclic amide bridged acidic
New Synthesis of Aryl and Heteroaryl N-Acylureas via Microwave-Assisted Palladium-Catalyzed Carbonylation
Chemistry (Weinheim an der Bergstrasse, Germany), 16(18), 5437-5442 (2010-04-09)
A protocol for the palladium(0)-catalyzed amidation of heteroaromatic tosylates was successfully developed. The methodology proved to be effective for a variety of heteroaryl tosylates including the pyridine, pyrimidine, quinoline and quinoxaline ring systems. Successful carbon-nitrogen bond formation with these heteroaryl
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