| 摘要 |
<p>Certain 3 min -substituted methyl nucleosides are disclosed which are useful in the treatment of viral infections, e.g., infections caused by herpes simplex virus types 1 and 2, and/or are useful as intermediates in the preparation of 3 min -substituted methyl nucleosides having antiviral activity. In accordance with one aspect of the invention, there are provided novel 3 min -substituted methyl nucleosides represented by Formulas I and II <CHEM> wherein: B indicates that B can be either alpha or beta; B is a member selected from the group consisting of the pyrimidine and purine nucleoside bases connected to the tetrahydrofuran ring through the N<1> heterocyclic nitrogen atom of the pyrimidines and the N<9> or N<7> heterocyclic nitrogen atom of the purines including the naturally occurring nucleoside bases and 5-fluoro, 5-bromo, 5-iodo, 5-chloro, 5-trifluoromethyl, 5-ethyl, 5-(2-bromovinyl)uracil; triazolecarboxamide; 2-aminopurine; 2,6-diaminopurine; 4-chloropyrimidine; pyrimidine; azapyrimidine; purine; 2,6-dichloropurine; 2-amino-6-chloropurine; and deazapurine; R and Q are either both hydrogen or halogen, especially fluorine, or one is hydrogen and the other one is hydroxy or halogen, especially fluorine; in Formula I at least one of R and Q is halogen; and X and Y can be the same or different and are selected from the group consisting of O-alkyl, O-aryl, O-acyl-, halogen, especially fluorine, azido, amino, acylamido, -SH, S-alkyl and S-aryl, or one of X or Y can be hydroxy, or X may be the group R<1>O and Y may be the group R<2>O wherein R<1> and R<2> are hydrogen or hydroxy-protecting groups. Preferred O-alkyl and S-alkyl groups contain from one to four carbon atoms; preferred O-aryl and S-aryl groups contain from 6 to 10 carbon atoms; and preferred O-acyl groups contain from one to four carbon atoms.</p> |
