Ru(II)-mediated Synthesis and Bioactivity Evaluation of 1,4,5- trisubstituted N-phthalimido Protected 5-bromo-1,2,3-triazolic Amino Acid

Recent Developments in the Ruthenium‐Catalyzed Azide Alkyne Cycloaddition (RuAAC) Reaction

“…Mucha and colleagues have reported the synthesis of 5‐bromo‐substituted‐1,4,5‐trisubstituted amino acid 24 in high yield using [Cp*RuCl(PPh 3 ) 2 ] (Scheme 17). [43] Following ester hydrolysis, the cytotoxicity of the resulting carboxylic acid was evaluated against two human cell lines (immortal human keratinocyte and skin fibroblast), with no effect on cell viability detected, indicating that this amino acid building block is well tolerated by human cells. Zhao and Burke Jr. attempted to modify an alkyne‐labeled peptide on solid phase via RuAAC with [Cp*RuCl(PPh 3 ) 2 ] as the catalyst, aiming to prepare polo‐like kinase inhibitors [44] .…”