| 摘要 |
PURPOSE: Provided is fields of organic chemistry, pharmaceutical chemistry and chemical manufacture, and a convenient and economical process for preparing benzo£f|quinolinones which are useful as 5 alpha -reductase inhibitors and provides intermediate compounds for the preparation of such pharmaceuticals. CONSTITUTION: 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-naphthoA2,3-dUthiazolyl, 2-naphtoA1,2-dUthiazolyl, 9-anthryl, 2-thiazolyl, 2-benzimidazolyl, 1-benzAgUisoquinolinyl, 8-benzAgUisoquinolinyl, 5-1H-tetrazolyl, 2-quinazolinyl, 2-thiazoloA4,5-bUpyridinyl, 4-10H-pyridazinoA3,2-bU-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 5 alpha -reductase.
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