首页> 外国专利> A procedure for the preparation of new 5-aroil-pirrol-2-carboxylic acids and derivatives of carboxylic acid. (Machine-translation by Google Translate, not legally binding)

A procedure for the preparation of new 5-aroil-pirrol-2-carboxylic acids and derivatives of carboxylic acid. (Machine-translation by Google Translate, not legally binding)

机译:一种制备新的5-芳基-吡咯-2-羧酸及其衍生物的方法。 (通过Google翻译进行机器翻译,没有法律约束力)

摘要

A procedure for the preparation of new 5-aroyl-pyrrole-2-carboxylic acids and carboxylic acid derivatives of general formula: **(See formula)** and the therapeutically useful salts of the corresponding carboxylic acids, where Ar is a phenyl group or a phenyl group substituted with one or more of the halogen, lower alkyl, lower alkoxy, nitro, amino, methylthio and cyano radicals and R3 represents a member selected from the group consisting of COOH, COO-lower alkyl, CONH2, CONH-lower alkyl and CON- (lower alkyl) 2, whose process is characterized by reacting a carboxylic acid halide of general formula: **(See formula)** where Ar'has the meaning given above to Ar except for the aminophenyl group, with a pyrrole derivative of general formula: **(See formula)** in the presence of a Lewis acid and a solvent and, if desired, subjecting the ester thus obtained of the general formula **(See formula)** to one or both of the following operations, in arbitrary order: a) hydrolysis to free carboxylic acid and, if desired, subsequent conversion of said acid to the corresponding amide with ammonia or with an appropriate lower alkylamine or di (lower alkyl) amine or treating said acid with a base, in order to convert said acid in a therapeutically useful sa b) in the case that Ar'is a nitrophenyl group, catalytically hydrogenate said product to give the corresponding compound in which Ar is aminophenyl. (Machine-translation by Google Translate, not legally binding)
机译:制备新的5-芳酰基-吡咯-2-羧酸和通式为羧酸的衍生物的方法:**(参见通式)**和相应羧酸的治疗上有用的盐,其中Ar为苯基或被卤素,低级烷基,低级烷氧基,硝基,氨基,甲硫基和氰基中的一个或多个取代的苯基,并且R 3表示选自COOH,COO-低级烷基,CONH2,CONH-低级的成员烷基和CON-(低级烷基)2,其方法的特征在于使通式为:**(参见式)**的羧酸卤化物与A'具有以上对Ar的含义,但氨基苯基除外在路易斯酸和溶剂的存在下,通式(**)的吡咯衍生物**(见通式)**,并且如果需要,对通式**(见通式)**的所得酯进行一种或两种以下操作以任意顺序进行:a)水解为游离羧基酸,如果需要,随后用氨水或适当的低级烷基胺或二(低级烷基)胺或将其用碱处理将所述酸转化为相应的酰胺,以便将所述酸转化为可治疗的盐; b)在Ar′为硝基苯基的情况下,将所述产物催化氢化以得到其中Ar为氨基苯基的相应化合物。 (通过Google翻译进行机器翻译,没有法律约束力)

著录项

  • 公开/公告号ES372615A1

    专利类型

  • 公开/公告日1972-02-16

    原文格式PDF

  • 申请/专利权人 MCNEIL LABORATORIES INC.;

    申请/专利号ES19690372615

  • 发明设计人

    申请日1969-10-16

  • 分类号C07D;A61K;

  • 国家 ES

  • 入库时间 2022-08-23 08:47:24

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