HEXOSYL NUCLEOSIDE DERIVATIVE

摘要

NEW MATERIAL:The hexosyl nucleoside derivative of formulaI(B is nucleic acid base; R1 is H, provided that when R2 is H, then R1 is NO2, NH2, CHO or CH2OH; R2 is H, provided that when R1 is H, R2 is CHO or CH2OH; when R1 is NO2 or NH2, then R3 is group of formula II, and when R1 or R2 is CHO or CH2OH, R3 is group of formula III), and its protected compound. EXAMPLE:2',3'-Dideoxy-3'-(S)-hydroxymethyluridine. USE:2'-Deoxynucleoside antagonist (nucleic acid metabolism inhibiting agent, enzymatic reaction inhibiting agent, antitumor agent, antiviral agent, etc.). PROCESS:For example, the 4- and 6-positions of 3'-deoxy-3'-nitro-beta-D-glucopyranosyluracil are protected with benzaldehyde, and the protecting groups are removed after converting the compound to 2,3-dideoxy derivative. The nitro group of the product is reduced to amino group, and diazotized. The product is converted to 3'-formyl derivative and then intramolecular hemiacetal derivative, and reduced with NaBH4 to obtain the exemplified compound.