申请人:Montedison S.p.A.
公开号:EP0076721A1
公开(公告)日:1983-04-13
A process is herein described for the preparation of carboxylic acids of formula (I):
wherein Ar represents either an aromatic or heteroaromatic group containing one ring or several rings, linked together, having overall up to 20 carbon atoms, preferably chosen from among: a phenyl-, naphthyl-, diphenyl-, and thienyl group also substituted with groups inert under reaction conditions, preferably chosen from alkyl, cycloalkyl and aryl groups, optionally substituted, by among other halogen, alcoxyl, phenoxyl and ketonic groups, and wherein n is an integer equal to 1 or 2, characterized in that a 1-halogen-1- arylethane of formula (II):
wherein Ar has the meaning already defined herein and X is CI or Br, is made to react with CO and an alkaline hydroxide in the presence of a cobalt hydrocarbonyl salt catalyst or at least one of its precursors, at a temperature comprised between about 20°C and 70°C under a pressure comprised between about 1 and 10 atmospheres, in a biphasic aqueous/ organic liquid system consisting of:
a) an aqueous phase containing the alkaline hydroxide;
b) an organic phase consisting of the initial halide of formula (II) dissolved in the organic solvent substantially unmixable with the alkaline aqueous phase, in the presence of an "onium" salt and of the cobalt salt catalyst or of at least one of its precursors.
The products thus obtained have particular use in the field of pharmaceutical products (such as analgesics, antipyretics, etc.), and as intermediates in chemical syntheses in general, in the field of high purity chemicals phytophar- maceutical products.
本文描述了一种制备式 (I) 羧酸的工艺:
其中 Ar 代表芳香族或杂芳香族基团,该基团包含一个环或多个环,连接在一起,总体上具有多达 20 个碳原子,最好从以下基团中选择:苯基、萘基、二苯基和噻吩基,也可被反应条件下的惰性基团取代,最好选自烷基、 环烷基和芳基,可选择被卤素基、烷氧基、苯氧基和酮基取代,其中 n 为等于 1 或 2 的整数,其特征在于,式(II)的 1-卤代-1-芳基乙烷:
其中 Ar 具有本文已定义的含义,X 为 CI 或 Br,在钴烃基盐催化剂或其至少一种前体存在下,在温度约为 20°C 至 70°C,压力约为 1 至 10 个大气压的双相水溶液/有机液体体系中,与 CO 和碱性氢氧化物反应:
a) 含有碱性氢氧化物的水相;
b) 有机相,由溶解在有机溶剂中的式 (II) 初始卤化物组成,基本上不与碱性水相混合,存在 "鎓 "盐和钴盐催化剂或其至少一种前体。
由此获得的产品在医药产品(如镇痛药、解热镇痛药等)领域,以及作为一般化学合成的中间体,在高纯度化学植物药产品领域具有特殊用途。