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    • 6. 发明授权
    • Process for producing carboxylic acid derivatives
    • 制备羧酸衍生物的方法
    • US5510506A
    • 1996-04-23
    • US392852
    • 1995-03-27
    • Akira TakaseHiroyuki KaiMoriyasu MasuiKatuhisa MasumotoAkihiko NakamuraYujiro KiyoshimaMikio Sasaki
    • Akira TakaseHiroyuki KaiMoriyasu MasuiKatuhisa MasumotoAkihiko NakamuraYujiro KiyoshimaMikio Sasaki
    • C07C249/12C07C251/48C07C229/02
    • C07C249/12C07C251/48
    • A process is disclosed to produce a carboxylic acid derivative of the general formula VIII!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and L are each as defined in the specification, characterized in that a benzyl halide is reacted with a cyano compound to give a phenylacetonitrile, which is then reacted with an alkyl nitrite in the presence of a base to give an .alpha.-hydroxyiminophenylacetonitrile, which is then reacted with an alkylating agent to give an .alpha.-alkoxyiminophenylacetonitrile, which is then hydrolyzed in the presence of a base, or is hydrated and treated with an acid, followed by hydrolysis in the presence of a base, to give an .alpha.-alkoxyiminophenylacetic acid, which is then reacted with an acid halide forming agent, or is convened into a metal salt, followed by reaction with an alkylating agent, or is reacted with a lower alcohol in the presence of an acid catalyst.According to the present invention, the reactions can be allowed to proceed under mild conditions over the whole process, and the desired carboxylic acid derivative VIII! can be produced without any facilities such as high-pressure steam equipment, high-temperature heat medium control equipment and freezing machines. In addition, there is no need to use various different solvents in the respective steps and the present process can be conducted with only one solvent, in which respect the present invention is also advantageous.
    • PCT No.PCT / JP94 / 01075 Sec。 371日期:1995年3月27日 102(e)1995年3月27日PCT PCT 1994年7月1日PCT公布。 出版物WO95 / 01328 日本公开1995年1月12日。公开了一种制备通式[Ⅷ]羧酸衍生物的方法:各自如说明书中所定义,其特征在于苄基卤与氰基化合物反应得到苯乙腈 然后在碱的存在下与亚硝酸烷基酯反应,得到α-羟基亚氨基苯基乙腈,然后与烷基化剂反应,得到α-烷氧基亚氨基苯基乙腈,然后在碱的存在下水解,或水合和 然后在碱的存在下水解,得到α-烷氧基亚氨基苯基乙酸,然后与酰卤化物形成试剂反应,或转入金属盐中,随后与烷基化剂反应, 或者在酸催化剂的存在下与低级醇反应。 根据本发明,可以在整个过程的温和条件下进行反应,并且可以制备所需的羧酸衍生物[Ⅷ],无需任何设备,例如高压蒸汽设备,高温热介质控制 设备和冷冻机。 此外,在各步骤中不需要使用各种不同的溶剂,并且本发明方法可以仅使用一种溶剂进行,其中本发明也是有利的。