Chlorambucil (1) is a chemotherapy drug that has been used in the treatment of leukemia, ovarian and breast cancer, and in various autoimmune diseases. Chlorambucil is an alkylating agent that binds to DNA and RNA preventing the replication of the cell. This drug is also known to be a carcinogen and teratogen. It is the objective of this investigation to synthesize analogs of chlorambucil while decreasing its toxicity. We have synthesized several analogs of chlorambucil; namely, compounds (3) and (4), derived from the chlorambucil acyl chloride (2). The structure of compounds 2, 3, and 4, were revealed by examination of ¹H and ¹³C NMR spectra.