鎮痛剤の合成研究(第55報)4a-(3-Substituted phenyl)-1,2-disubstituted Decahydrocinnoline誘導体の合成その2(複素環式化合物の合成研究第955報)

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With the expectation of the synthesis of the compounds having both agonist and antagonist properties, novel decahydrocinnoline derivatives (IIa-i), (IIIa-g) and (IVa-f) were synthesized as analgetics. In order to prepare N-2-propenyl derivatives, the reduction of N-acryloyl compounds (IIf) and (IIg) with various reducing agents (lithium aluminum hydride, sodium borohydride and sodium bis (2-methoxyethoxy) aluminum hydride was examined. In addition, it was found that N-acryloyl derivative (IIf) cyclized to give 2,3,4,5,6,6a, 7,8,9,10,10a, 11-dodecahydro-1H-pyrazolo [1,2-a] cinnoline derivative (VII) by heating with phosphorus pentasulfide and potassium sulfide in xylene. Among these decahydrocinnoline derivatives (IVa), (IVb) and (IVc) were found to have a potent analgesic effect with antagonistic effect for morphine analgesia.
社団法人日本薬学会の論文
1982-02-25