Polysubstituted pyrimidinylphosphonic and 1,3,5-triazinylphosphonic acids with potential biological properties were prepared in high yields by the microwave-assisted Michaelis-Arbuzov reaction of trialkyl phosphite with the corresponding halopyrimidines and halo-1,3,5-triazines, respectively, followed by the standard deprotection of the phosphonate group using TMSBr in acetonitrile. 4,6-Diamino-5-chloropyrimidin-2-ylphosphonic acid () was found to exhibit a weak to moderate anti-influenza activity (28-50 μM) and may represent a novel hit for further SAR studies and antiviral improvement.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7125588 | PMC |
| http://dx.doi.org/10.1016/j.tet.2011.11.040 | DOI Listing |
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