In order to look for novel antitumor drugs and virucides with high activity and low toxicity, a series of amino acid linked phosphoryl nitrogen mustard derivatives have been synthesized. The structures of all compounds prepared were confirmed by 1H NMR, 31P NMR, IR, MS spectroscopy, and elemental analyses. In the case of dl‐α‐amino acid derivatives, the presence of multiple chiral centers in the target products leads to the generation of diastereoisomers, which can be detected by spectroscopic and analytical (TLC) methods. Preliminary bioassays indicate that some of compounds 5 have high inhibitory activities against some tumor cells and tobacco mosaic virus (TMV). In addition, some of them display certain herbicidal activities and significant fungicidal activities against wheat leaf rust.
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