申请人:Hoechst Aktiengesellschaft
公开号:US04797409A1
公开(公告)日:1989-01-10
New 1-hydroxy-2-pyridones of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3, which are identical or different, denote hydrogen or lower alkyl having 1-4 carbon atoms, R.sup.1 and R.sup.3 preferably being hydrogen, and R.sup.2 preferably being methyl, X denotes S or, preferably, O, Y denotes hydrogen or up to 2 halogen atoms, namely chlorine and/or bromine, Z denotes a single bond or the bivalent radicals O, S, --CR.sub.2 -- (R=H or C.sub.1 -C.sub.4 -alkyl) or other 2-valent radicals with 2-10 carbon and, optionally, oxygen and/or sulfur atoms linked to form a chain, it being obligatory when the radicals contain 2 or more oxygen and/or sulfur atoms for the latter to be separated by at least 2 carbon atoms, and it being possible for 2 adjacent carbon atoms also to be linked together by a double bond, and the free valencies of the carbon atoms being saturated by H and/or C.sub.1 -C.sub.4 -alkyl groups, Ar denotes an aromatic ring system which has up to two rings and can be substituted by up to three radicals from the group comprising fluorine, chlorine, bromine, methoxy, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl and trifluoromethoxy, are prepared by a variety of process variants. The compounds and their physiologically tolerated salts with inorganic or organic bases mainly have antimycotic, anti-bacterial and antiviral activity. The compounds of the formula V ##STR2## in which R.sup.1, R.sup.2, R.sup.3, X, Y, Z and Ar have the same meaning as in formula I, which occur in the preparation of the compounds of the formula I, are also new.
通式I中的新1-羟基-2-吡啶酮如下:##STR1## 其中R1、R2和R3相同或不同,表示氢或具有1-4个碳原子的低烷基,其中R1和R3优选为氢,R2优选为甲基,X表示S或O,Y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价基团,具有2-10个碳原子和可选的氧和/或硫原子,形成链,当基团含有2个或更多的氧和/或硫原子时,后者必须由至少2个碳原子分离,并且也可能通过双键将2个相邻的碳原子连接在一起,碳原子的自由价通过H和/或C1-C4-烷基基团饱和,Ar表示芳香环系统,最多有两个环,并且可以被来自氟、氯、溴、甲氧基、C1-C4-烷基、三氟甲基和三氟甲氧基的最多三个基团取代,通过多种方法变体制备的化合物及其与无机或有机碱的生理耐受盐主要具有抗真菌、抗细菌和抗病毒活性。通式V中的化合物如下:##STR2## 在制备通式I中的化合物时,其中R1、R2、R3、X、Y、Z和Ar的含义与通式I中相同。