The synthesis, structure and biological activities of a series of derivatives of normorphine, noracetylmethadol (IV a), 6-amino-4,4-diphenyl-3-heptanol acetate (V a), and norpropoxyphene (VI a), in which the corresponding nitrogen supports an alkylating group (chloroethyl or fumaroyl) are reported. Structural identification was achieved spectroscopically. 13C Nuclear Magnetic Resonance proved the most useful tool in this task. N-Chloroethylnoracetylmethadol (IV c), acted as a potent long-lasting analgesic. Although some compounds (IV c), (V c) and (V d) showed substantial cytostatic activity, no antineoplastic activity in mice with P388 leukaemia was detected in the series.