| 摘要 |
<p>1,189,761. Phenoxyalkanoic acids. MERCK & CO. Inc. 8 Jan., 1968 [11 Jan., 1967], No. 1123/68. Heading C2C. Novel compounds I (including salts, esters and amides thereof) wherein R signifies alkyl, cycloalkyl, alkenyl, carboxy-alkyl, amino-alkyl, amino substituted carboxy-alkyl, hydroxy-alkyl, alkanoyl, aryl, carboxy substituted-aryl, or aralkyl; R<SP>1</SP> and R<SP>2</SP> which may be the same or different signify alkyl, aryl or aralkyl; the X radicals which may be the same or different signify hydrogen, halogen, alkyl and when taken together two X radicals on adjacent carbons of the benzene ring may be joined to form a hydrocarbon chain containing 4 carbons between their points of attachment; m is an integer of from 1 to 4 and n is 1, 2 or 3; are prepared by the interaction of a compound of the formula (Ph represents a benzene ring substituted by Xm) or an ester or amide thereof, and a mercaptan RSH; esters and amides may also be obtained from the corresponding free acid by standard methods and if the above interaction is carried out in the presence of a base the product is a salt. 2,3 - Dichloro - 4 - (2,2 - diacetylvinyl) - phenoxy-acetyl chloride, obtained from the corresponding phenoxy-acetic acid utilizing thionyl chloride, is converted the corresponding phenoxy-acetamide by treatment with anhydrous ammonia. Ethyl 3 - (2,2 - diacetylvinyl) - 4 - chloro - phenoxy-acetate is obtained by reacting acetylacetone with ethyl 3-formyl-4-chloro-phenoxyacetate (hydrolysis of the diacetyl compound affords the corresponding phenoxy-acetic acid); ethyl 2,3 - dichloro - 4 - (2,2 - diacetylvinyl) - phenoxy-acetate, ethyl 2-[2,3-dichloro-4-(2,2-diacetylvinyl)-phenoxy-propionate and the corresponding free acids are similarly obtained. Twelve similar esters and the corresponding free acids are tabulated. Pharmaceutical preparations showing diuretic and saluretic action contain as active ingredient compounds I; administration may be orally or by intravenous injection.</p> |
