Abstract The selectivity of the formation of N-di (2-chloroethyl) methylamine in reactions with various chlorinating agents has been investigated and the optimum chlorinating agent has been found. 1-Amino-4-methylpiperazine has been obtained for the first time by the cyclization of N-di (2-chloroethyl) methylamine with aqueous hydrazine. A possible mechanism has been proposed for the cyclization reaction.