循環器系薬の合成研究(第4報)縮環ジヒドロピリジン誘導体の合成

概要

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1,4,5,6-Tetrahydropyrrolo [3,4-b] pyridin-7-ones (III) and 2,5,5,7,7-pentamethyl-1,4,5,7-tetrahydrofuro [3,4-b] pyridines (XII) were synthesized from 4-benzylidene-2,3-dioxopyrrolidines (I) or 4-benzylidene-2,2,5,5-tetramethyltetrahydrofuran-3-ones (XI), respectively, to find new cardiovascular drugs. Their 1,4-dihydropyridine structures were confirmed from spectral data and by oxidation to the corresponding pyridines. It was also found that Madhav's intermediate was not 1,4-dihydropyridine (III) but 4-(3-amino-2-ethoxycarbonyl-1-phenyl-2-butenyl)-2,3-dioxopyrrolidine (II_1). 1,4,5,6-Tetrahydropyrrolo [3,4-b]-pyridin-7-ones possessing 6-ω-aminoalkyl substituent (VII) were obtained from 6-ω-hydroxyalkyl derivatives (V) by the usual way. These compounds were tested for coronary vasodilating and antihypertensive activities, and several of them showed a marked coronary vasodilating activity.
公益社団法人日本薬学会の論文
1978-04-25