首页> 外国专利> METHOD OF OBTAINING SUBSTITUTED BENZENOSULPHONYLMONATE12 The invention relates to a method for producing new benzenesulfonylureas of the general formula X-CO-TSTH-CH with, -CH 2 - ^ ^amp; - SO ^ -NH-CO-NH - / ^)

METHOD OF OBTAINING SUBSTITUTED BENZENOSULPHONYLMONATE12 The invention relates to a method for producing new benzenesulfonylureas of the general formula X-CO-TSTH-CH with, -CH 2 - ^ ^amp; - SO ^ -NH-CO-NH - / ^)

机译:获得取代的苯磺酰基甲酸酯的方法本发明涉及一种生产通式为X-CO-TSTH-CH的新的苯磺酰脲的方法,其具有-CH 2-^>&-SO ^ -NH-CO-NH-/ ^)。

摘要

1,233,354. Benzenesulphonyl-ureas. FARBWERKE HOECHST A.G. 14 Feb., 1969 [2 Aug., 1968], No. 8218/69. Heading C2C. Novel compounds I (including salts thereof) wherein X signifies the groups II or III in which R signifies C 1-4 alkyl, Z signifies halogen, C 1-4 alkyl or C 1-4 alkoxy and ZSP1/SP signifies halogen or C 1-4 alkyl are obtained according to standard methods. N - [4 - (# - Aminoethyl) - benzenesulphonyl]. NSP1/SP - (#SP2/SP - cyclohexenyl) - urea is prepared by saponifying the #-acetamidoethyl-compound. 1 - [4 - (# - 2 - Methoxy - 5 - chlorobenzamido - ethyl) - benzenesulphonyl] - 3 - (#2. cyclohexenyl)-parabanic acid is prepared by the interaction of 1-(#2-cyclohexenyl)-parabanic acid and 4 - (# - 2 - methoxy - 5 - chlorobenzamido - ethyl) - benzenesulphochloride. #2 - Cyclohexenyl isocyanate is prepared by heating N - (#2 - cyclohexenyl) - NSP1/SP,NSP1/SP - diphenyl-urea. The cyclohexenylamine salt of N-[4 - (# - 2- methoxy - 5 - chlorobenzamido - ethyl) - benzenesulphonyl] - NSP1/SP - aceryl - urea is obtained by mixing the individual compounds and heating. N - (#2 - Cyclohexenyl) - carbamic acid phenyl ester is prepared by the interaction of phenyl chloroformate and #2-cyclohexenylamine. N - Acetyl - NSP1/SP - (#2 - cyclohexenyl) - urea is prepared by the interaction of acetic anhydride and #2-cyclohexenyl-urea. N,N - Diphenyl - NSP1/SP - (#2 - cyclohexenyl)- urea is prepared from diphenyl carbamoyl chloride and #2-cyclohexenylamine. N,NSP1/SP - Di - (#2 - cyclohexenyl) - urea is prepared from #2 - cyclohdxenyl isocyanate and #2-cyclohexenylamine. N - [4 - (# - 2 - Methoxy - 5 - chlorobenzamido - ethyl) - benzenesulphonyl] - phenylurethane, -NSP1/SPNSP1/SP - diphenyl - urea, - iminodithio - carbonic acid potassium salt and dimethyl ester, -NSP1/SP - (#2 - cyclohexenyl) - isothiourea methyl ether, -NSP1/SP-(#2-cyclohexenyl)- thiourea and - NSP1/SP - (#2 - cyclohexenyl) - isourea methyl ether and 4-(#-2-methoxy-5-chlorobenzamido - ethyl) - benzene sulphonamide are also prepared as intermediates. Pharmaceutical preparations exhibiting blood sugar lowering properties and hypoglycemic activity contain I as active ingredient; administration is orally.
机译:1,233,354。苯甲磺酰脲。法伯克·霍赫斯特(FARBWERKE HOECHST A.G。),1969年2月14日[1968年8月2日],编号8218/69。标题C2C。新颖的化合物I(包括其盐),其中X表示基团II或III,其中R表示C 1-4烷基,Z表示卤素,C 1-4烷基或C 1-4烷氧基和Z 1 表示卤素或C 1-4烷基根据标准方法获得。 N-[4-(#-氨基乙基)-苯磺酰基]。通过将#-乙酰氨基乙基化合物皂化来制备N 1 -(# 2 -环己烯基)-脲。 1-[4--(#-<2-甲氧基-5-氯苯甲酰胺基>-乙基)-苯磺酰基]-3-(#2。环己烯基)-对羟基苯甲酸通过1-(#2-环己烯基)-的相互作用制备顺丁烯二酸和4-(#-<2-甲氧基-5-氯苯甲酰胺>-乙基)-苯磺酰氯。 #2-环己烯基异氰酸酯是通过加热N-(#2-环己烯基)-N 1 ,N 1 -二苯基脲制备的。 N- [4--(#-<2-甲氧基-5-氯苯甲酰胺基>-乙基)-苯磺酰基]-N 1 -丙烯酰基-脲的环己烯胺盐是通过混合各个化合物并加热获得的。 N-(#2-环己烯基)-氨基甲酸苯酯是通过氯甲酸苯酯和#2-环己烯基胺的相互作用制备的。 N-乙酰基-N 1 -(#2-环己烯基)-尿素是通过乙酸酐与#2-环己烯基-脲的相互作用制备的。 N,N-二苯基-N 1--(#2-环己烯基)-脲是由二苯基氨基甲酰氯和#2-环己烯基胺制备的。 N,N 1--二-(#2-环己烯基)-脲是由#2-环己烯基异氰酸酯和#2-环己烯基胺制备的。 N-[4-(#-<2-甲氧基-5-氯苯甲酰胺基>-乙基)-苯磺酰基]-苯基氨基甲酸酯,-N 1 N 1 -二苯基-尿素, -亚氨基二硫代-碳酸钾盐和二甲基酯,-N 1 -(#2-环己烯基)-异硫脲甲基醚,-N 1 -(#2-环己烯基) -硫脲和-N 1 -(#2-环己烯基)-异脲甲基醚和4-(#-<2-甲氧基-5-氯苯甲酰胺基--乙基)-苯磺酰胺也被制备为中间体。具有降血糖特性和降血糖活性的药物制剂中,I为有效成分。口服给药。

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