133956-94-2Relevant academic research and scientific papers
A convenient approach to hydroxyethylene dipeptide isosteres as building blocks for enzyme inhibitors
Radunz, Hans-Eckart,Eiermann, Volker,Schneider, Guenther,Riethmueller, Angelika
, p. 1887 - 1894 (2007/10/02)
γ-Lactones 6,8,10 and the ester 9, precursors to the hydroxyethylene dipeptide isostere unit, were synthesized stereoselectively in two or three steps from α-amino-ketones in good yield. Peptides containing these isosteres are potent inhibitors of certain aspartyl proteinases. Alkylation of the (3S,4S)substituted γ-lactone 6 afforded exclusively cis-alkylation, with regard to C-2 and C-4.
