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    • 6. 发明公开
    • Synthesis of benzo(f)quinolinones
    • 苯并(F)chinolinone-SYNTHESE
    • EP0839807A1
    • 1998-05-06
    • EP97308644.0
    • 1997-10-29
    • ELI LILLY AND COMPANY
    • Brennan, JohnDoecke, Christopher WilliamHeath, Perry ClarkPatterson, Lawrence EdwardUdodong, Uko EffiongWeigel, Leland Otto
    • C07D221/10C07C323/22
    • C07D417/12C07C319/14C07C319/20C07C323/22C07C2602/10C07D221/10C07C323/21C07C323/38C07C323/62
    • A process for preparing intermediates and benzoquinolin-3-one pharmaceuticals, of the following formula I:
      wherein R 1 represents:
      2-nitrophenyl, 4-nitrophenyl, 2-cyanophenyl, 4-cyanophenyl, 2-nitronaphthyl, 4-nitronaphthyl, 2-cyanonaphthyl, 4-cyanonaphthyl, 2-quinolinyl, 4-quinolinyl, 7-quinolinyl, 1-isoquinolinyl, 3-isoquinolinyl, 8-isoquinolinyl, 2-quinoxalinyl, 2-benzothiazolyl, 3-1H-indazolyl, 2-benzoxazolyl, 3-1,2-benzisothiazolyl, 2-pyridinyl, 4-pyridinyl, 2-pyrazinyl, 2-naphtho[2,3-d]thiazolyl, 2-naphto[1,2-d]thiazolyl, 9-anthryl, 2-thiazolyl, 2-benzimidazolyl, 1-benz[g]isoquinolinyl, 8-benz[g]isoquinolinyl, 5-1H-tetrazolyl, 2-quinazolinyl, 2-thiazolo[4,5-b]pyridinyl, 4-10H-pyridazino[3,2-b]-2-quinazolinyl, 2-1,4-benzodioxinyl, 2-triazine, 2-benzoxazine, 4-benzoxazine, 2-purine or 8-purine.
      Such pharmaceuticals are effective in treating conditions consequent on 5α-reductase.
    • 制备下式I的中间体和苯并喹啉-3-酮药物的方法:其中R 1表示:2-硝基苯基,4-硝基苯基,2-氰基苯基,4-氰基苯基,2-硝基萘基,4 2-硝基萘基,2-氰基萘基,4-氰基萘基,2-喹啉基,4-喹啉基,7-喹啉基,1-异喹啉基,3-异喹啉基,8-异喹啉基,2-喹喔啉基,2-苯并噻唑基,3-1H-吲唑基, - 苯并恶唑基,3-1,2-苯并异噻唑基,2-吡啶基,4-吡啶基,2-吡嗪基,2-萘并[2,3]恶噻唑基,2-萘并[1,2]噻唑基,9-蒽基,2-噻唑基,2-苯并咪唑基 ,1-苯并异喹啉基,8-苯并异喹啉基,5-1H-四唑基,2-喹唑啉基,2-噻唑并[4,5-b]吡啶基,4-10H-哒嗪基-3,3,2-b] -2-喹唑啉基,2-1,4-苯并二恶英基,2 3-三嗪,2-苯并恶嗪,4-苯并恶嗪,2-嘌呤或8-嘌呤。 这样的药物在治疗5α-还原酶的病症方面是有效的。