Optimal Lipophilicity of Sulfonium p-Toluenesulfonate as Anti-allergic Drug

Abstract

In the development of the anti-allergic drug Suplatast Tosilate (IPD-1151T) we have reported the QSAR analysis using only the calculated π values, because the few logK values of sulfonium compounds had been measured till then. In this study, we measured the logK_TLC value of sulfonium compounds by using octylsililated silicagel plate (Merck HPTLC RP-8 F_254S). The logK_TLC values of the optimized compounds 52 and 67 (Suplatast Tosilate) of dimethylsulfonium p-toluenesulfonates derivatives were 0.07 and 0.06, respectively. Therefore, it was found that the desirable logK_TLC value of the sulfonium compound was approximately zero as the anti-allergic drug.