SYNTHESIS OF MEXILETINE ANALOGUES

Five types of derivatives related to 1-(2,6-dimethylphenoxy)amino-propane have been synthesized. They are phenoxy-aminopropane (Ⅲ,Ⅴ), phenoxy-hydroxy-aminopropane (Ⅵ), N-acyl-phenoxy-aminoisopropane (Ⅶ), phenoxy-isopropyl ester of benzoic acid (Ⅷ) and phenoxy-isopropyl-ammonium salts (Ⅸ).In preliminary pharmacological assay, some of these compounds exhibited obvious effect of decreasing heart rate on the isolated toad heart. Ⅲ a～c were shown to be more active than mexiletine.In addition, some of the compounds Ⅲa～b, Ⅳa～b, and VIb were found to possess anticonvulsant activity.