Synthesis of saccharidyl N,N‐bis(2‐chloroethyl)phosphoramidates and their antitumor activity

Publisher Website
Google Scholar
Abstract
In order to search for novel antitumor drugs with high activity and low toxicity, a series of new compounds, galactopyranosyl (or glucofuranosyl) N,N‐bis(2‐chloroethyl) phosphoramidates, have been synthesized. The structures of all compounds prepared were proved by 1H NMR, 31P NMR, IR, and MS spectroscopy and by elemental analyses. The existence of diastereoisomers was detected by 31P NMR and 1H NMR spectra. One of the two isomers of 3a and also one of 4b, i.e., 3a′ and 4b′, respectively, were obtained by recrystallization. The absolute configurations of 3a′ and 4b′ were determined by single‐crystal X‐ray diffraction analysis. The results of the preliminary biological tests indicated that some of these compounds have certain inhibitory activities against L1210 cells.