2-Chloro-2'-deoxy-6-O-methylinosine is used as a reagent in the preparation of 2-chloro-2'-deoxyadenosine analogs via regioselective and stereoselective glycosylation of 6-(substituted-imidazol-1-yl)purines with 2-deoxy-3,5-di-O-(p-toluoyl)-α-D-erythro-pentofuranosyl chloride.