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method of preparation of aryloxyacetiques thiolesters and new aryloxyacetiques thiolesters

机译:芳氧基乙酸硫酯的制备方法和新的芳氧基乙酸硫酯

摘要

1421104 Aryloxyacetic thiolesters J BLUM 29 April 1974 [4 May 1973] 18576/74 Heading C2C The invention comprises novel compounds of the general Formula (I): where Ph is an optionally substituted aryl group; R is an organic radical containing neither phenol nor mercaptan groups; RSP1/SP is a hydrogen atom or hydrocarbon radical, preferably aliphatic; and RSP11/SP is an aliphatic, cycloaliphatic, aromatic or heteroaromatic group, which is not aliphatic, when RSP1/SP is hydrogen. In particular, the group SR is a group derived from (N-acetyl) homocystein, (N-acetyl) cystein, beta-mercaptoethanol, parachlorophenoxy-2-isobutyryl-O-mercaptoethanol or carboxymethylmercaptan. The compounds are made by process (a) in which an aqueous solution of a metallic salt of a mercaptan reacts with an optionally substituted aryloxyacetic acid halide of the formula PhOCRSP1/SPRSP11/SPCOX, where X is halogen, or process (b) in which a substituted aryloxyacetic acid halide reacts with a mercaptan in an inert, neutral or basic organic medium, and the mercaptan and possibly phenol group or groups contained in the mercaptan react with the substituted aryloxyacetic acid halide. Pharmaceutical preparations having hypolipemic, hypocholesteiolemic, hepatoprotective, tonic, healing and mucolytic effects contain (I) as active ingredient. Administration is orally, rectally or parenterally.
机译:1421104芳氧基乙酸硫代酯J BLUM 1974年4月29日[1973年5月4日] 18576/74标题C2C本发明包含通式(I)的新化合物:其中Ph是任选取代的芳基; R是既不含有苯酚也不含有硫醇基团的有机基团; R 1 是氢原子或烃基,优选脂族基;当R 1 为氢时,R 11 为脂族,脂环族,芳族或杂芳族基团,不是脂族基。特别地,基团SR是衍生自(N-乙酰基)高半胱氨酸,(N-乙酰基)半胱氨酸,β-巯基乙醇,对氯苯氧基-2-异丁酰基-O-巯基乙醇或羧甲基硫醇的基团。这些化合物是通过方法(a)制备的,其中硫醇金属盐的水溶液与任选取代的式PhOCR 1 R 11 的芳氧基乙酸卤化物反应其中X为卤素的COX或方法(b),其中取代的芳氧基乙酸卤化物在惰性,中性或碱性有机介质中与硫醇反应,并且硫醇以及硫醇中可能包含的酚基团与取代基反应芳氧基乙酸卤化物。具有降血脂,降胆固醇,保肝,滋补,愈合和粘液溶解作用的药物制剂含有(I)作为活性成分。口服,直肠或肠胃外给药。

著录项

  • 公开/公告号BE814365A

    专利类型

  • 公开/公告日1974-08-16

    原文格式PDF

  • 申请/专利权人

    申请/专利号BE19746044563

  • 发明设计人 J. BLUM;

    申请日1974-04-29

  • 分类号C07C;

  • 国家 BE

  • 入库时间 2022-08-23 06:15:04

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