| 摘要 |
1337280 5 - Phenyl -isoxazole - 3 - carboxylic acid derivatives FERLUX 30 Nov 1970 [23 Dec 1969] 56782/70 Heading C2C Novel compounds I in which (1) R 2 , R 3 , R 4 and R 5 are H and R 1 is OH; (2) R 1 , R 2 , R 4 and R 5 are H and R 3 is H, OH alkyl, halo, alkoxy, acetoxy or NO 2 ; (3) R 2 and R 5 are H, R 1 and R 3 are OH or OCH 3 and R 4 is H or OCH 3 ; or (4) R 1 , R 4 and R 5 are H and R 2 and R 3 are OCH 3 and R is OH, NR 6 R 7 , N<SP>1</SP>-(R 8 )-piperazino, -NH-NHR 9 , guanidino or OR 10 ; R 6 and R 7 are H, alkyl, haloalkyl, optionally substituted aryl, cycloalkyl or cyanoalkyl; R 8 is hydroxyalkyl; R 9 is H, alkyl, aryl, or arylalkyl and R 10 is dialkylaminoalkyl, alkyl or pyridylalkyl and their salts are prepared by (1) reaction of hydroxylamine hydrochloride with an acid II in which R 1 is other than OH, (2) reaction of hydroxylamine with an acid IV in the presence of a sodium alcoholate, (3) reaction of the appropriate acid chloride with a suitable amine or alcohol or (4) reaction of the free acid with an alcohol R 10 OH. (3,4 - Dimethoxybemoyl)pyrtivic acid is prepared by reaction of 3,4-dimethoxy-acetophenone with ethyl oxalate. Pharmaceutical compositions useful as salidiuretics comprise a compound I together with a suitable diluent or carrier and are administered orally or parenterally. Some compounds I also have analgesic, sedative, hypotensive or hypertensive properties.
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