Synthesis of Biologically Active 1-Arylethylphosphonates

Autor: Gulyukina, N., Dolgina, T., Bondarenko, G., Beletskaya, I., Bondarenko, N., Henry, J., Lavergne, D., Ratovelomanana-Vidal, V., Genet, J.
Zdroj: Russian Journal of Organic Chemistry; April 2002, Vol. 38 Issue: 4 p573-587, 15p
Abstrakt: A convenient and inexpensive general preparation method for 1-arylethylphosphonic acids and their esters was developed involving in reduction of the corresponding 1-ethenylphosphonates by ammonium formate in the presence of palladium on carbon. A homogeneous enantioselective hydrogenation of 1-arylethenylphosphonic acids in the presence of chiral ruthenium catalysts provided optically active 1-arylethylphosphonic acids of enantiomeric purity up to 86%. The preliminary data on biological activity testing of the 1-arylethylphosphoic acids synthesized evidence that some among the compounds obtained are low-toxic substances with the properties of immunosuppressors of the central type of action.
Databáze: Supplemental Index