| 摘要 |
PURPOSE:To prepare the titled compound useful as pharmaceuticals, suppressing the side reactions, in high yield, by reacting 3,4-dimethoxyphenetylamine with the reaction product of an acetophenone derivative and thionyl halide, and subjecting the product to the reductive desulfurization reaction. CONSTITUTION:The acetophenone derivative of formulaI(R<2> is H, alkanoyl, or aralkyl) is made to react with thionyl halide, and the reaction product is made to react with the 3,4-dimethoxyphenethylamine to obtain the thioacetamide derivative of formula II. The objective compound of formula V can be prepared by the reductive desulfurization reaction of the compound of formula II. The compound of formula II may be alkylated to the acetophenone derivative of formula III (R<3> is alkyl), or reduced and alkylated to the benzyl alcohol derivative of formula IV (R<1> is H or aralkyl) before the reductive desulfurization reaction. The compound of formula III used as an intermediate is an easily purifiable stable compound, and can be purified and separated extremely easily.
|
