| 摘要 |
<p>Pyrazole derivs. of formula (I) and their salts are new: In (I) X is S or O. R1 is H or, on any available position, one or more, same or different, 1-4C alkyl, alkoxy or alkylthio, halo, CF3, NO2, COOH, 1-4C alkoxy-carbonyl, di(1-4C alkyl)amino or amidino. R2 and R3 are each 1-4C alkyl, 5-7C cycloalkyl, benzyl or phenyl, the last opt. substd. by R1. R3 can also be H. R4 is H, 1-4C alkyl (opt. substd. by di(1-4C alkyl)amino, COOH, 1-4C alkoxycarbonyl, CN or imidazolin-2-yl), imidazolin-2-yl, or CO(CH2)nR5. n = 0-2. R5 is Cl, 1-4C alkoxy (opt. substd. by di(1-4C) alkylamino) or, where n = 0, NH2, opt. alkylated or acylated hydrazino. R5 can also be NR6R7. R6 and R7 are each H, 1-6C alkyl (opt. substd. by OH, and/or mono- or di-(1-4C) alkylamino), or together with N complete a 5-8 membered ring which may contain an additional O, S or N atom or is substd. by 1-4C alkyl (opt. itself substd. by OH, ethylenedioxy, trimethylenedioxy) or phenyl). (I) have uricosuric and uricostatic activities, sometimes associated with a diuretic effect. They are also analgesics, antiphlogistics, antidepressants and cardiac/circulatory (e.g. antiarrhythmic agents). (IV) are intermediates but also have analgesic and antiphlogistic properties. In an example, 3-Me-1-Ph-benzo b -1H-pyrazolo 4,3-f 1,4 -oxazepine was prepd. from 5-Cl-3-CH3-1-Ph-pyrazole-4-aldehyde and O-NH2-phenol, and was reduced (NaBH4) to the 4,5-dihydro analogue.</p> |
