Copper-Catalyzed Alkynylation of Hydrazides: An Easy Access to Functionalized Azadipeptides
We 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.
OL2022-6614GreenAccess1.pdf
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OL2022-6614GreenAccess.pdf
postprint
embargo
2023-09-06
copyright
8.05 MB
Adobe PDF
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