Synthesis and biological evaluation of novel difluorophenyl methanesulfinyl acetamide derivatives

Based on the study results of known structure-activity relationships(SARs) of modafinil derivatives,a series of difluorophenyl methanesulfinyl acetamide compounds were designed and synthesized,and their central stimulative activities were investigated.The target compounds were synthesized starting from dis(4-fluorophenyl) methanol by substitution,esterification,amination and oxidation. Sixteen target compounds( 5a-5p ) were synthesized and their structures were confirmed by ESI-MS,¹H NMR,IR and elemental analysis. Their central stimulative effects were evaluated by the independent activity assay in mice. Preliminary results of pharmacological test showed that compounds 5a,5b,5c,5e and 5j enhanced activities of healthy mice,and the central stimulative activity of 5b was comparable to that of the positive control modafinil.