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[摘要]：Polymer-supported O6-(benzotriazol-1-yl)inosine derivs. (Pol-I and Pol-dI) have been synthesized reasonably effectively via reaction of nucleoside phosphonium salts with polymer-linked HOBt (Pol-HOBt). In contrast to soln. chem., use of polymer-supported BOP (Pol-BOP) did not lead to efficient nucleoside loading. Presence of the nucleosides on the support could be readily detected by MAS NMR. Exposure of the polymer-supported nucleosides, Pol-I and Pol-dI, to alc., phenol, thiol and amine nucleophiles caused cleavage from the support leading directly to the C-6 modified nucleoside analogs, e.g. I. These are the first examples of the application of such technol. for nucleoside modification. Where possible, results of reactions with the polymer-supported nucleosides are compared to those from soln. chem., providing insight into the differences between the two techniques. These new polymer-supported nucleosides can be conveniently utilized for diversity-oriented synthesis. |
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