1-hydroxy-2-pyridones, a process for their preparation, and...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/89 (2006.01) A61K 31/44 (2006.01) C07D 309/38 (2006.01)

Patent

CA 1302415

H0E 86/F 081K Abstract of the disclosure: New 1-hydroxy-2-pyridones of the general formula I Image in which R1, R2 and R3, which are identical or different, denote hydrogen or lower alkyl having 1 - 4 carbon atoms, R1 and R3 preferably being hydrogen, and R2 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, -CR2- (R = H or C1-C4-alkyl) or other 2-valent radical 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 C1-C4-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, bro- mine, methoxy, C1-C4-alkyl, trifluoromethyl and trifluoromethoxy, 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 antiviral activity. The compounds of the formula V Image in which R1, R2, R3, 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.

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