| 摘要 |
1,127,188. Organic compounds. J. R. GEIGY A.G. 29 Dec., 1965 [30 Dec., 1964], No. 55018/65. Heading C2C. Novel compounds of the general formula wherein X represents hydrogen, halogen up to the atomic number 35, the trifluoromethyl radical or an alkyl, alkanoyl, alkoxy, alkyl. sulphonyl or dialkylsulphamoyl radical, having at most 4 C atoms in each alkyl radical, Y represents hydrogen or the acyl radical of a carboxylic acid, A represents an alkylene radical having 2-5 carbon atoms in a straight or branched chain and R represents a C 1-4 alkyl radical or A and R together represent an alkane triyl radical having at most 8 carbon atoms in a straight or branched chain, which radical with #N-O-Y forms a C-pyrrolidinyl-alkyl, C- piperidylalkyl or C - hexahydroazepinylalkyl radical substituted at the nitrogen atom by -O-Y and optionally substituted at carbon atoms by alkyl radicals, and their salts with inorganic and organic acids, are prepared by reacting a secondary amine of the general formula wherein X, A and R have the meanings given above with an acyl peroxide the reaction being performed in an inert solvent at a temperature of at most 20‹ C. and in the presence of an acid binding agent to form an N-acyloxy compound embraced by first general formula above wherein Y represents a monoacyl radical, if desired, hydrolysing this N-acyloxy compound and, if desired, converting the N-hydroxy compound obtained into an acid addition salt or into another O-acyl derivative embraced by the general Formula I. Pharmaceutical preparations in conventional form for oral, rectal, topical or parenteral administration comprise a compound of the first general formula above and at least one inert pharmaceutical carrier.
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