Le Du, EliottBorrel, JulienWaser, Jerome2022-09-222022-09-222022-09-222022-09-0610.1021/acs.orglett.2c02625https://infoscience.epfl.ch/handle/20.500.14299/190871We report a copper-catalyzed alkynylation of azadipeptides using ethynylbenziodoxolone (EBX) reagents. Nonsymmetrical ynehydrazides could be obtained in 25–97% yield using azaglycine derivatives as nucleophiles. The transformation is compatible with most functional groups naturally occurring on amino acid side chains and allows the transfer of silyl-, alkyl-, and aryl-substituted alkynes. The obtained α-alkynyl azaglycine products could be further functionalized by nucleophilic attack or cycloaddition on the triple bond.text::journal::journal article::research article