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    • 87. 发明公开
    • Process for the preparation of alpha-aryl-propionic acids and their alkaline salts
    • Verfahren zur Herstellung von alpha-Aryl-propionsäurenund deren Alkalisalzen。
    • EP0076722A1
    • 1983-04-13
    • EP82401703.2
    • 1982-09-20
    • Montedison S.p.A.
    • Gardano, AndreaFrancalanci, FrancoFoa', Marco
    • C07C51/10C07C57/30C07C57/58C07C59/64C07C51/41B01J31/28
    • C07C51/10C07C57/30C07C59/64C07C57/58
    • A process is described for the preparation of alpha-aryl-propionic acids and their alkaline salts having the formula (I):
      wherein Ar represents an aromatic, heteroaromatic group containing one or several rings linked together, having overall up to 20 carbon atoms, preferably chosen from amongst phenyl-, naphthyl-, diphenyl- and thienyl groups, these in turn being possibly substituted by groups inert under reaction conditions, preferably chosen from amongst: alkyl-, cycloalkyl- and aryl- groups optionally substituted, halogens, alkoxyl groups, phenoxyl groups, ketone groups, by reaction with carbon monoxide of the corresponding secondary halides of formula (II):
      wherein: Ar has already been defined, while X is a halogen chosen from Cl or Br, and which process is characterized in that the reaction is conducted in an anhydrous alcohol solvent consisting of alkanols having up to 4 carbon atoms, in the presence of alkaline hydroxides, and in the further presence of a cobalt hydrocarbonyl salt, optionally supported on resins, or of one of its precursors, at a temperature comprised between 0°C and 50°C and under substantially atmospheric pressure.
      The products thus obtained have a particular use in the field of pharmaceutics (analgesics, antipyretics, etc.) and as intermediates for chemical syntheses in general in the field of high-purity chemicals, and of phytodrugs.
    • 描述了用于制备具有式(I)的α-芳基丙酸及其碱性盐的方法:... ...其中Ar表示含有连接在一起的一个或多个环的芳族杂芳族基团,其总体上至 20个碳原子,优选选自苯基 - ,萘基 - 二苯基 - 和噻吩基,这些反应可能被反应条件下惰性的基团取代,优选选自烷基 - ,环烷基 - 和芳基 - 任选取代的卤素 烷氧基,苯氧基,酮基,通过与相应的次级卤化物式(II)的一氧化碳反应:... 其中:Ar已经被定义,而X是选自Cl或Br的卤素,以及 该方法的特征在于反应在碱性氢氧化物存在下,在具有至多4个碳原子的链烷醇组成的无水醇溶剂中进行,并且在进一步存在ac 任选负载在树脂上,或其前体之一的烃基盐,在0℃至50℃的温度和基本上大气压下。 这样得到的产品在药物领域(止痛剂,解热剂等)和作为高纯度化学品领域的化学合成的中间体以及植物药物领域具有特别的用途。