SYNTHESIS OF 4-(AND 5-)-t-BUTYL-2-(2-DIMETHYLAMINO) ETHOXYPHENYL DIMETHYLCARBAMATES AS REVERSIBLE CHOLINESTERASE INHIBITORS

Two title compounds, which are nuclear alkylated ortho isomers of CUI XING AN, were prepared and tested for anticholinesterase activity and other actions. Preliminary results indicated that introduction of a t-butyl group on the benzene ring lowered toxicity and anticholinesterase activity.Monoetherification of 4-t-butyl pyrocatechol with 2-dimethylamino ethyl chloride yielded a mixture of 4-t-butyl and 5-t-butyl-2-(2-dimethylamino) ethoxy phenol (Ⅳ₁ and Ⅳ₂) in approximately equal proportions. The hydro chlorides of the two isomers could be separated by fractional crystallization from methanol. Their structures were characterized.