A new method for synthesis of nucleoside-5'-phosphonates containing a reactive halogen atom in the phosphonate residue has been developed. In order to achieve selective inhibition of individual enzymes and to elucidate the structure of their active sites, the synthesis of 5-'chloromethyl-, 5'-(beta-bromoethyl)-and 5'-(N-chloroacetylaminomethyl)-phosphonate esters of adenosine and previously unknown analogous derivatives of uridine have been carried out. The method described may also be used to synthesize 5'-phosphonate esters of nucleosides, which contain radioactive labels.
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