Efficient synthesis of fluorothiosparfosic acid analogues with potential antitumoral activity

In this paper, we describe a short synthesis of N-(phosphonoacetyl)-l-aspartate (PALA) analogues. The mono- and difluorinated thioacetamide precursors were prepared in one step from methyl (diethoxyphosphono)di- and monofluoromethyldithioacetates 8 and 11 as starting materials. Antiproliferating properties on a L1210 strain and ATCase inhibition of these new compounds are disclosed. ThioPALA(FF) 5c showed a remarkable cytotoxic activity towards murine leukemia L1210, when used as tetraester.

Ester thioPALA(FF), prepared in one step, showed a remarkable cytotoxic activity towards murine leukemia L1210 cell.Figure optionsDownload as PowerPoint slide