首页> 外国专利> method the blood cholesterol lowering and gallstones muodo stu preventive phenoxy - isovoihappoesterien fluorijohdannaisten val assembly.

method the blood cholesterol lowering and gallstones muodo stu preventive phenoxy - isovoihappoesterien fluorijohdannaisten val assembly.

机译:方法降血脂和预防胆结石预防苯氧基-异硫杂多酯荧光素的组装。

摘要

1,218,817. Fluoroderivatives of phenoxyisobutyric acid esters. SOC. D'ETUDES SCIENTIFIQUES ET INDUSTRIELLES DE L'lLEDE-FRANOE. 22 Aug., 1968 [26 Sept., 1967; 22 Dec., 1967], No. 40281/68. Heading C2C. Novel compounds of the formula in which R is a straight or branched chain C 1-5 alkyl radical, and X is a CF 3 -, CF 3 S-, CF 3 S(O)-, or CF 3 SO 2 - radical, are obtained by treating an X-substituted phenol with chloroform and acetone in the presence of potash to form the corresponding phenoxy isobutyric acid which is then converted into an ester by a C 1-5 alkanol. The following intermediates are also described p-Nitrotribromomethylbenzene is obtained by reacting p-nitrotoluene with bromine; p-trifluoromethylnitrobenzene is obtained by treating the previous product with SbF 3 ; p-trifluoromethylaniline is obtained by reducing the previous product with SnCl 2 ; p-trifluoromethylphenol is obtained by diazotizing and hydrolysing the previous product. p-Nitrophenylmethyl sulphide is obtained by reacting p-chloronitrobenzene with Na 2 S followed by refluxing with dimethylsulphate, then the product is chlorinated to form p-nilrophenyl trichloromethyl sulphide, which is reacted with SbF 3 to form p-nitrophenyl trifluoromethyl sulphide and the latter is reduced with SnCl 2 in HCl to yield p-aminophenyltrifluoromethyl sulphide; the latter is diazotized and hydrolysed to p-hydrophenyltrifluoromethylsulphide; p-trifluoromethylsulphinylphenoxy isobutyric acid is obtained by oxidizing p-trifluoromethylthiophenoxy isobutyric acid with sodium metaperiodate; p-trifluoromethylsulphonylphenoxy isobutyric acid is obtained by refluxing ptrifluoromethylthiophenoxy isobutyric acid dissolved in a mixture of acetic acid and oxygenated water for 3 hours. Pharmaceutical compositions useful as hypocholesterolemiants and biliary lithiasis preventatives comprise compounds of the above formula in the form of capsules or jelly pills.
机译:1,218,817。苯氧基异丁酸酯的氟代衍生物。 SOC。法兰西-法兰西德工业大学。 1968年8月22日[1967年9月26日; 1967年12月22日],第40281/68号。标题C2C。式中的新化合物,其中R为直链或支链C 1-5烷基,X为CF 3-,CF 3 S-,CF 3 S(O)-或CF 3 SO 2-基,通过在钾盐的存在下用氯仿和丙酮处理X-取代的苯酚以形成相应的苯氧基异丁酸,得到相应的苯氧基异丁酸,然后将其通过C 1-5链烷醇转化成酯,得到氯丁酮。还描述了以下中间体,对硝基三溴甲基苯是通过对硝基甲苯与溴反应制得的。对三氟甲基硝基苯是通过将先前的产物用SbF 3处理而获得的。对三氟甲基苯胺是通过用SnCl 2还原先前的产物而获得的。对三氟甲基苯酚是通过重氮化和水解先前的产物而获得的。对硝基苯基甲基硫化物是通过使对氯硝基苯与Na 2 S反应,然后与二甲基硫酸盐回流而获得的,然后将产物氯化以形成对硝基苯基三氯甲基硫化物,然后使其与SbF 3反应以生成对硝基苯基三氟甲基硫化物,而后者用SnCl 2在HCl中还原,得到对氨基苯基三氟甲基硫醚。后者被重氮化并水解为对-氢苯基三氟甲基硫化物。对-三氟甲基亚磺酰基苯氧基异丁酸是通过用偏高碘酸钠氧化对-三氟甲基硫代苯氧基异丁酸得到的。对三氟甲基磺酰基苯氧基异丁酸是通过将溶于乙酸和氧化水混合物中的对三氟甲基硫代苯氧基异丁酸回流3小时而获得的。用作降胆固醇药和预防胆结石的药物组合物包括胶囊或软糖丸形式的上式化合物。

著录项

  • 公开/公告号FI49151B

    专利类型

  • 公开/公告日1974-12-31

    原文格式PDF

  • 申请/专利权人 SOC ETUDES SCIENTIFIQUES ET INDFR;

    申请/专利号FI19680002613

  • 发明设计人 BULTEAU GFR;

    申请日1968-09-17

  • 分类号C07C69/66;

  • 国家 FI

  • 入库时间 2022-08-23 04:40:43

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