SYNTHESIS OF A NOVEL SERIES OF ARYLMETHYLISOTHIOURONIUM DERIVATIVES

The bromination by N-bromosuccinimide of various mesitylene derivative s, to produce arylmethyl bromides or bromoarylmethyl bromides was comp ared in different reaction conditions. These compounds are intermediat es in the synthesis of arylmethylisothiouronium bromide salts, achieve d by the quantitative addition of thiourea to the methyl bromide deriv atives. The final products are potent inhibitors of trans-membrane cat ion transport, and are therefore of potential interest for pharmacolog ical properties. The incorporation of a radioactive carbon, important for the use as affinity labels and stoichiometric studies, is demonstr ated.