Betaadrenolytically effective substances consisting of 1-aryloxy-3-alkylamino-2-propanols of the general formula I
wherein R¹ is alkyl with 3 to 4 carbon atoms, and R² is a ramified alkyl with 3 to 4 carbon atoms, such substances being prepared in a reaction in a polar solvent from
(a) alkyl ester of 3-acetyl-4[(3-bromo-2-hydroxy)-propoxy]phenylcarbamic acid with a primary alkylamine;
(b) alkyl ester of 3-acetyl-4[(2-3,epoxy)-propoxy]phenylcarbamic acid with a primary alkylamine in the medium of an alkanol with 1 to 3 carbon atoms;
(c) alkyl ester of 3-acetyl-4-hydroxyphenylcarbamic acid with 1-alkylamino-2,3-epoxypropane, the reaction being catalyzed by an alkali metal hydroxide; and
(d) alkyl ester of 3-acetyl-4-hydroxyphenylcarbamic acid with 1-alkylamino-3-chloro-2-propanol, the reaction being catalyzed by an alkali metal hydroxide.
由通式 I 的 1-芳氧基-3-烷基
氨基-2-
丙醇组成的β-
肾上腺素有效物质
其中 R¹ 为 3 至 4 个碳原子的烷基,R² 为 3 至 4 个碳原子的柱齿烷基,这类物质在极性溶剂中通过以下反应制备而成
(a) 3-乙酰基-4[(3-溴-2-羟基)-丙氧基]
苯基氨基甲酸与
伯胺的烷基酯;
(b) 3-乙酰基-4[(2-3,环氧)-丙氧基]
苯基氨基甲酸与一级烷基胺在 1 至 3 个碳原子的烷醇介质中的烷基酯;
(c) 3-乙酰基-
4-羟基
苯基氨基甲酸与 1-烷基
氨基-2,3-环氧
丙烷的烷基酯,该反应由碱
金属氢氧化物催化;及
(d) 3-乙酰基-
4-羟基
苯基氨基甲酸与 1-烷基
氨基-3-
氯-2-
丙醇的烷基酯,该反应由碱
金属氢氧化物催化。