ChemInform Abstract: Structure-Affinity Relationships of 12-Sulfonyl Derivatives of 5,8,8a, 9,10,11,12,12a,13,13a-Decahydro-6H-isoquino(2,1-g)(1,6)naphthyridines at α-Adrenoceptors.
Abstract
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ChemInform Abstract
LDA-mediated coupling of the dihydroisoquinolines (I) with the nicotinamide (II) forms the tetrahydroisoquinonaphthyridinones (III). Catalytical hydrogenation followed by reduction of the lactam and reaction with sulfonyl chlorides such as (IV) yields the diastereomeric decahydroisoquino(1,6)naphthyridines (V) - (VII) mentioned in the title. The derivative (Vb) is found to be a potent . alpha.2-adrenoceptor antagonist in vivo. Yields are only partly given.
