| 摘要 |
1,134,816. [4 - (2 - Nitro - 1 - alkenyl)- aryloxy] alkanoic acids and derivatives. MERCK & CO. Inc. 15 Nov., 1966 [22 Nov., 1965], No. 51083/66. Heading C2C. Novel compounds of the formula where R is an alkyl radical, X is a halogen atom or an alkenyl, aryloxy, aralkoxy or hydroxyalkyl radical, and n is 1, 2 or 3; and the pharmacologically acceptable salts, esters and amides thereof, are prepared by reacting a corresponding formylphenoxyalkanoic acid or ester with a primary amine and reacting the intermediate formed with a nitroalkane or aryl-substituted nitroalkane, and, if desired hydrolysing any ester group to the acid. Correspondingly the acid may be reacted with a base to form a salt, or with an alcohol to form an ester; or the acid may be converted to the acid chloride and reacted with an alcohol to form an ester or with ammonia or a monoalkylamine, dialkylamine, dialkylaminoalkylamine or heterocyclic amine to form an amide. The amide may also be obtained by reacting an ester with similar amines. Ethyl - (2 - (or 3 -) - chloro . 4 - formylphenoxy) acetate is obtained by reacting 2- (or 3-) chloro - 4 - hydroxy - benzaldehyde with ethyl bromoacetate. Pharmaceutical compositions having diuretic and saluretic effect comprise a compound of the above formula, or a salt, ester or amide thereof, together with a pharmaceutically acceptable diluent, carrier or coating in the form of tablets or capsules. |
