1.
Bioorg Med Chem Lett
; 13(19): 3351-4, 2003 Oct 06.
Article
in English
| MEDLINE
| ID: mdl-12951124
ABSTRACT
The asymmetric synthesis of novel, potent phosphoramidate alpha(2-6)sialyltransferase transition-state analogue inhibitors such as (R)-9 (K(i)=68 microM) is described, via condensation of cytidine phosphitamide 6 with key chiral, non-racemic alpha-aminophosphonates, prepared in >98% ee by Mitsunobu azidation followed by Staudinger reduction of the corresponding chiral, non-racemic alpha-hydroxyphosphonates.