| 摘要 |
The invention relates to a A method for making osyl and hexoses derivatives of formula 1 , especially 2-fluoro-2-deoxy derivatives.
wherein R is a nucleoside such as adenosine, cytidine, guanosine, uridine and deoxy analogs such as 2-deoxy, X represents OH, halogen, particularly F, NH 2 Y represents H, CH 2 OH, CH 2 NH 2 , CH 2 OPO 3 , CH 2 OSO 3 Z represents O or S, and W represents O, NH, or CH 2 ,
said method comprising the steps of: a) stereoselective fluorophosphorylation of tetrapivaleate 8
to give ²-gluco-type fluorophosphate, b) hydrogenation and deprotection to give a monophosphate, c) coupling said glycal with (R)P-morpholidate to give crude sugar nucleotide 1 , or alternatively, d)deacetylation then silylation of heptaglycal 7
to give tetrasilylated glycal, e) fluorophosphorylation of said glycal to give ²-gluco type fluorophosphate, f) deprotection of the fluorophosphate and coupling radical R to give 1 . Use of said derivatives as inhibitors of highly virulent proteins of pathogenic bacteria.
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