Antihypertensive isoindolinyl-amino-imidazoline - prepd. by reacting 2-amino-isoindoline with 2-alkylthio-2-imidazoline

摘要

2-(Isoindolin-2-ylamino)-2-imidazoline of formula (I) and its physiologically tolerable acid addn salts are new. When administered orally or parenterally, (I) has strong and long-lasting antihypertensive activity. Dosage is 1-10 mg/kg per day. In an example, (II) (15g) and 2-methylthio-2-imidazoline hydriodide (26.9g) in n-amyl alcohol (200 ml) are refluxed 30 mins., then evaporated. The residue is partitioned between CH2Cl2 and water. The organic phase is sepd. off and evaporated. The residue was extracted with hot benzene, and the resulting solid residue is treated with 2-N NaOH, filtered off and recrystallised from benzene to give pure (I) (8.4g), m.pt. 160-162 degrees C.