More than hundred compounds from aziridine class shown certain biological activity. We report here the synthesis of racemic version of protected azidomethyl aziridine via easily accessible intermediates. Further, small combinatorial library of triazolylmethyl aziridines was obtained by CuAAC reaction and deprotection. To the best of our knowledge such aziridine derivatives have not been tested for their biological activities. Comparison of synthesis of racemic and enantiomerically pure series of products and their biological activities will be discussed.