| 摘要 |
Novel sulphonamides of the formula wherein X is a straight or branched chain hydrocarbon radical of 1-4 carbon atoms, A is an alkyl, cycloalkyl, aryl (e.g. phenyl or naphthyl), haloaryl, phenylmercaptoalkyl, alkoxyaryl, alkoxyhaloaryly, phenoxyalkyl, dealkoxyaryl, alkylaryl, or haloalkylaryl radical and R1 is an alkyl, cycloalkyl, aryl, haloaryl, aralkyl, alkoxy, alkoxyalkyl or alkoxyalkoxy radical, are made by (a) reacting a corresponding benzene sulphur chloride compound of the formula A.CO.NH.X.C6H4.S.(O)n.Cl wherein n is 0, 1 or 2 with a 2-aminopyrimidine, and if necessary, oxidizing the product to form the -SO2NH-grouping; (b) reacting a corresponding benzenesulphonyl guanidine with a compound of the formula Y-CO-CHR1-CO-Y1 wherein Y and Y1 are hydrogen atoms or alkoxy radicals, or with functional derivatives thereof and, when the product contains a hydroxy substituent in the 4- and/or 6-position of the pyrimidine ring, converting to the corresponding halogen compound and subjecting this to reductive dehalogenation; (c) acylating the appropriate amino-substituted benzenesulphonyl-pyrimidine with a reactive derivative of an acid of the formula A.COOH; (d) reacting the appropriate benzenesulphonamide with a pyrimidine derivative bearing a reactive ester substituent, e.g. a halogen atom, or a trialkylamino group, in the 2-position, or (e) reacting the appropriate benzenesulphonic acid with a 2-acetylamino-pyrimidine. 4 - (b - Benzamido - ethyl) - benzenesulphonyl guanidine is made by reacting 4-b -benzamido-ethyl-benzenesulphonamide with guanidine carbonate. a - Isobutyl - b - dimethylamino - acrolein is made by treating isobutyl-acetaldehyde diethyl acetal with dimethyl formamide and phosgene in methylene chloride. a - Phenyl - b - chloroacrolein is made by treating phenylacetaldehyde diethyl acetal with phosgene and dimethyl formamide and reacting the resulting a - phenyl - b - dimethylamino-acrolein with phosgene.
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