| Summary: | Functionally 4,6-disubstituted 1<i>H</i>-pyrazolo[3,4-<i>d</i>]pyrimidines are important compounds with various pharmacological activities. 1-Substituted 4-chloro-6-(chloromethyl)-1<i>H</i>-pyrazolo[3,4-<i>d</i>]pyrimidines are practically unexplored derivatives in this series. In this paper, it was shown that the nucleophilic substitution of 4-Chloro-6-(chloromethyl)-1-methyl-1<i>H</i>-pyrazolo[3,4-<i>d</i>]pyrimidine with methylamine produced selectively 4-substituted product, 6-(chloromethyl)-<i>N</i>,1-dimethyl-1<i>H</i>-pyrazolo[3,4-<i>d</i>]pyrimidin-4-amine. The structure of the synthesized compound was established by elemental analysis, high resolution mass-spectrometry, <sup>1</sup>H, <sup>13</sup>C-NMR, and IR spectroscopy, mass-spectrometry, and X-ray analysis.
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