| 摘要 |
PURPOSE:To obtain the titled compound useful as a remedy for circulatory diseases easily and economically on an industrial scale in high yield by one-step reaction without producing hardly separable by-product, by reacting deacetylmoxisylyte with acetic anhydride in the presence of hydrochloric acid. CONSTITUTION:Deacetylmoxisylyte of formula I {=[2-(4-hydroxy-2-isopropyl-5- methylphenoxy)ethyl]-dimethylamine} (abbreviated as DAM) is made to react with acetic anhydride in the presence of hydrochloric acid at 60-120 deg.C for 0.5-3hr. After the completion of the reaction, the reaction liquid is concentrated and dried under reduced pressure an the precipitated crystal is separated e.g. by filtration to obtain the objective compound of formula II having activity to suppress sympathetic nerve. The hydrochloric acid is preferably concentrated hydrochloric acid and its amount is preferably equimolar amount or somewhat excess, e.g. 1.2-2.0mol per 1mol of DMA. EFFECT:The amounts of reagent and solvent can be remarkably decreased and the production process can be simplified.
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