首页> 外国专利> 1-HYDROXY-2-PYRIDONES, A PROCESS FOR THEIR PREPARATION, AND MEDICAMENTS WHICH CONTAIN THEM, AND INTERMEDIATES FORMED IN THE PREPARATION OF THE 1-HYDROXY-2-PYRIDONES

1-HYDROXY-2-PYRIDONES, A PROCESS FOR THEIR PREPARATION, AND MEDICAMENTS WHICH CONTAIN THEM, AND INTERMEDIATES FORMED IN THE PREPARATION OF THE 1-HYDROXY-2-PYRIDONES

机译:1-羟基-2-吡咯烷酮及其制备方法和包含它们的药物,以及在制备1-羟基-2-吡咯烷酮时所用的中间体

摘要

H0E 86/F 081KAbstract of the disclosure:New 1-hydroxy-2-pyridones of the general formula Iin whichR1, R2 and R3, which are identical or different, denotehydrogen or lower alkyl having 1 - 4 carbon atoms,R1 and R3 preferably being hydrogen, and R2preferably being methyl,X denotes S or, preferably, O,Y denotes hydrogen or up to 2 halogen atoms, namelychlorine and/or bromine,Z denotes a single bond or the bivalent radicals O, S,-CR2- (R = H or C1-C4-alkyl) or other 2-valentradical with 2 - 10 carbon and, optionally, oxygenand/or sulfur atoms linked to form a chain, it beingobligatory when the radicals contain 2 or more oxygenand/or sulfur atoms for the latter to be separatedby at least 2 carbon atoms, and it being possible for2 adjacent carbon atoms also to be linked togetherby a double bond, and the free valencies of thecarbon atoms being saturated by H and/or C1-C4-alkylgroups,Ar denotes an aromatic ring system which has up to tworings and can be substituted by up to three radicalsfrom the group comprising fluorine, chlorine, bro-mine, methoxy, C1-C4-alkyl, trifluoromethyl andtrifluoromethoxy, are prepared by a variety of pro-cess variants. The compounds and their physiologi-cally tolerated salts with inorganic or organic- 2 -bases mainly have antimycotic, anti-bacterial and antiviralactivity. The compounds of the formula Vin which R1, R2, R3, X, Y, Z and Ar have the samemeaning as in formula I, which occur in the preparationof the compounds of the formula I,are also new.
机译:H0E 86 / F 081K公开摘要:通式I的新的1-羟基-2-吡啶酮在其中R1,R2和R3相同或不同,表示氢或具有1-4个碳原子的低级烷基,R1和R3优选为氢,并且R2最好是甲基X表示S或OY表示氢或最多2个卤素原子,即氯和/或溴,Z表示单键或二价基团O,S,-CR2-(R = H或C1-C4-烷基)或其他2价含2-10个碳和氧的自由基和/或硫原子连接形成链,自由基含有2个或更多氧时必须和/或硫原子以便后者分离至少有两个碳原子,并且有可能2个相邻的碳原子也要连接在一起通过双键和自由价碳原子被H和/或C1-C4-烷基饱和组,Ar表示最多具有两个的芳环系统环,最多可被三个基团取代选自氟,氯,溴地雷,甲氧基,C1-C4-烷基,三氟甲基和三氟甲氧基,是由多种亲cess变体。这些化合物及其生理无机或有机的愈伤组织耐受盐-2-碱主要有抗霉菌,抗菌和抗病毒活动。式V化合物其中R1,R2,R3,X,Y,Z和Ar具有相同的在制剂中出现的含义如式I式I化合物也是新的。

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