SYNTHESIS OF CATECHOL AMINOKETONE AND ITS ANALOGUES

In this paper, the synthesis of a series of aminoketone derivatives are reported.Compounds Ⅰ_1～9 and Ⅱ_1～10 were synthesized from substituted chloroacetophenone with various amines. Compounds Ⅰ_10～12 and Ⅱ_11～12 were synthesized from substituted acetophenones with corresponding amines through Mannich reaction. The ¹HNMR and MS were discussed. Pharmacological study showed that the vascular contraction of dog ruesenteric and basilar arteries induced by serotonine and calcium in vitro could not be antagonized by this kind of compounds and the known compound 3,4-dihydroxy acetophenone (Ⅰ₀) Except Ⅰ₁₀, the vasodilator effects of all compounds as shown by measurement of arterial blood flow after injection into femoral artery in dogs are weaker than Ⅰ₀. After intravenous injection in anesthetized dogs, Ⅰ₁₀ showed the same effect as Ⅰ₀ to increase coronary blood flow and myocardial contraction. Furthermore, the ventricular arrhythmia induced by aconitine and chloroform could also be protected by compound Ⅰ₁₀, but compound Ⅰ₀ was not effective.