ヘテロ環縮合Isoquinolone誘導体の合成研究(第2報)Thiazinoisoquinolone誘導体の合成と薬理作用

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11-Dimethylaminomethyl-3,4-dihydro-6-oxo-2H, 6H-1,3-thiazino [3,2-b] isoquinoline (IVa) and 11-formyl-3,4-dihydro-6-oxo-2H, 6H-1,3-thiazino [3,2-b] isoquinoline (VI) were synthesized by Mannich reaction and Vilsmeier reaction of 3,4-dihydro-6-oxo-2H, 6H-1,3-thiazino [3,2-b] isoquinolone (I), respectively. 6-Oxo-4H, 6H-1,3-thiazino [3,2-b] isoquinoline (XIb) was synthesized from 2-acetoxy-3,4-dihydro-6-oxo-2H, 6H-1,3-thiazino [3,2-b] isoquinoline (IXb) upon treatment with p-tolenesulfonic acid, which was prepared by the Pummerer reaction of I. Reaction of 3,4-dihydro-6-oxo-2H, 6H-1,3-thazino [3,2-b] isoquinoline-1,1-dioxide (III) with alkyl halides gave monoalkylated (XIII) and dialkylated derivatives (XIV). The anti-inflammatory activity of these compounds was tested by the rat carrageenin paw edema method. IXa, b and VI showed stronger activity than phenylbutazone.
公益社団法人日本薬学会の論文
1979-10-25