Stereoselective synthesis of phosphoramidate α(2-6)Sialyltransferase transition-State analogue inhibitors

The asymmetric synthesis of novel, potent phosphoramidate α(2-6)sialyltransferase transition-state analogue inhibitors such as ( R)- 9 ( K i=68 μM) is described, via condensation of cytidine phosphitamide 6 with key chiral, non-racemic α-aminophosphonates, prepared in >98% ee by Mitsunobu azidati...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (19), p.3351-3354
Hauptverfasser:	Skropeta, Danielle, Schwörer, Ralf, Schmidt, Richard R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - pharmacology Carbohydrates. Nucleosides and nucleotides Chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Exact sciences and technology Nucleosides, nucleotides and oligonucleotides Organic chemistry Phosphoric Acids - chemical synthesis Phosphoric Acids - pharmacology Preparations and properties Sialyltransferases - chemical synthesis Sialyltransferases - pharmacology Stereoisomerism
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