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Synthesis of a TMC-95A Ketomethylene Analogue by Cyclization via Intramolecular Suzuki Coupling

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journal contribution
posted on 27.08.2003, 00:00 authored by Markus Kaiser, Carlo Siciliano, Irmgard Assfalg-Machleidt, Michael Groll, Alexander G. Milbradt, Luis Moroder
A TMC-95A analogue extended at the C-terminus with NleΨ[COCH2]Gly-Ala-Ala-NH2 was synthesized via side-chain cyclization of the linear precursor by a Suzuki cross-coupling reaction in solution to analyze the effect of additional P‘ residues on the inhibitory potency against yeast proteasome.