| 摘要 |
PURPOSE:To industrially and advantageously obtain the titled compound useful as an agent for hypertension, angina pectoris, arrhythmia, etc., by reacting a 1-p-carboxymethylphenoxy-2,3-epoxypropane with isopropylamine using a phase-transfer catalyst. CONSTITUTION:A compound expressed by formula II (Ar is aryl) [e.g. 2.epoxy-3-[p-beta-methoxyethyl)-phenoxy-propane] is reacted with isopropylamine in the presence of a phase-transfer catalyst expressed by formula I (R' is alkyl, R is benzyl or alkyl; X is halogen or sulfate) (e.g. tetramethylammonium chloride) to afford a propanol derivative (e.g. atenolol expressed by formula IV) expressed by formula III. The compound expressed by formula III is useful as a selective blocker for cardiac sympathetic beta-receptors. The reaction can be carried out at about ambient temperature in high yield in a short time without using a special apparatus by this method. |
