发明名称 Antiarrhythmic 1-phenoxy-3-aminoethoxy-2-propanol derivs. - prepd. by reacting 1-phenoxy-2,3-epoxy-propane cpds. with 2-amino-ethanol cpds.
摘要 <p>New aminoethoxyphenoxypropanol derivs are cpds., of formula (I) and their salts with acids:- In formula (I), R is CH3, OCH3 or OC2H5; and A is diisopropylamino, or piperidino. (I) are useful as antiarrhythmic agents. Their activity is demonstrated in tests against arrhythmia induced by infusion of aconitine into rats at a rate of 5 mu/kg/min. The duration of infusion before the occurrence of the first ventricular extrasystole is measured, and the dosage of test cpd., required to increase this time by 50% is reported as the D150. In this test, (I; R = OCH3, A = diisopopylamino) has an ED150 of 5.57 mg/kg i.v., while the known cpd., 1-(2-diethylaminoethoxy)-3-(o-methoxyphenoxy)-2-propanol HCl has an ED150 of 13.5 mg/kg i.v. Specific cpds., (I) include 1-(2-pyrrolidinoethoxy)-3-(o-methoxyphenoxy)-2-propanol. In an example, this is prepd. in 36% yield by reacting 1,2-epoxy-3-(o-methoxy-phenoxy)propane with pyrrolidinoethanol.</p>
申请公布号 DE2639733(A1) 申请公布日期 1978.03.09
申请号 DE19762639733 申请日期 1976.09.03
申请人 DR. CHRISTIAN BRUNNENGRAEBER CHEMISCHE FABRIK & CO MBH 发明人 RICHTER,HELMER,DR.-ING.
分类号 C07D295/092;C07D303/22;C07D303/24;(IPC1-7):07D295/08;61K31/445 主分类号 C07D295/092
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