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    • 2. 发明申请
    • NEW METHOD FOR N-CYCLOPROPYLATION OF AROMATIC AMINES, AS WELL AS COMPOUNDS AND COMPOSITIONS OBTAINED
    • 新方法用于芳族化合物的N-环丙烷化作为化合物和组合物获得
    • WO9502573A2
    • 1995-01-26
    • PCT/HU9400025
    • 1994-07-12
    • SOMFAI EVA
    • SOMFAI EVA
    • C07C227/08C07D215/56A61K31/495C07D215/36
    • C07D215/56C07C227/08
    • Process for the introduction of a cyclopropyl group into a primary or secondary aromatic amine or into heterocyclic compounds containing a secondary nitrogen atom reacting to the corresponding amines or their salts so as to form the corresponding N-cyclopropyl-(1'-carboxy)-derivatives either with the reagent of general formula (I), optionally in the presence of an acid binding agent or with 2,4-dihalogen-butyric acid ester or with chloroacetic acid ester, whereupon the resulting N-(alkoxy-carbonyl)-methyl-derivative is treated with alkali alkylate and dihalogen-ethane to convert the alkoxy-carbonyl-methyl group into a carbalkoxy-cyclopropyl group and subsequently optionally hydrolysing the ester groups if present and optionally eliminating the 1'-carboxyl group introduced in the course of the first step, whereby the last step is carried out optionally after introducing other substituents into the aromatic ring or after eliminating other substituents from the aromatic group. The method is suitable to synthesize 1-cyclopropyl-7-piperazine-1,4-dihydro-quinolone-3-carboxylic acid derivatives. New biologically active compounds are formed including compounds of formula (IV) and their salts which are used in pharmaceutical and veterinary compositions.
    • 将环丙基引入伯或仲芳族胺或含有与相应胺或其盐反应的仲氮原子的杂环化合物中以形成相应的N-环丙基 - (1'-羧基) - 衍生物的方法 任选地在酸结合剂或2,4-二卤代丁酸酯或氯乙酸酯的存在下,与通式(I)的试剂反应,由此得到的N-(烷氧羰基) - 甲基 - 衍生物用碱性烷基化物和二卤代乙烷处理以将烷氧基羰基 - 甲基转化为烷氧基 - 环丙基,随后任选地水解酯基(如果存在的话),并且任选地除去在第一个过程中引入的1'-羧基 其中最后一步可任选地在将其它取代基引入到芳环中之后或在从芳族基团中除去其它取代基之后进行。 该方法适用于合成1-环丙基-7-哌嗪-1,4-二氢喹诺酮-3-羧酸衍生物。 形成新的生物活性化合物,包括用于药物和兽药组合物的式(IV)化合物及其盐。
    • 3. 发明专利
    • CHEMICAL PROCEDURE AND MATERIALS
    • HU9302005D0
    • 1993-10-28
    • HU9302005
    • 1993-07-13
    • SOMFAI EVA
    • SOMFAI EVA
    • C07C227/08C07D215/56
    • Process for the introduction of a cyclopropyl group into a primary or secondary aromatic amine or into heterocyclic compounds containing a secondary nitrogen atom reacting to the corresponding amines or their salts so as to form the corresponding N-cyclopropyl-(1'-carboxy)-derivatives either with the reagent of general formula (I), optionally in the presence of an acid binding agent or with 2,4-dihalogen-butyric acid ester or with chloroacetic acid ester, whereupon the resulting N-(alkoxy-carbonyl)-methyl-derivative is treated with alkali alkylate and dihalogen-ethane to convert the alkoxy-carbonyl-methyl group into a carbalkoxy-cyclopropyl group and subsequently optionally hydrolysing the ester groups if present and optionally eliminating the 1'-carboxyl group introduced in the course of the first step, whereby the last step is carried out optionally after introducing other substituents into the aromatic ring or after eliminating other substituents from the aromatic group. The method is suitable to synthesize 1-cyclopropyl-7-piperazine-1,4-dihydro-quinolone-3-carboxylic acid derivatives. New biologically active compounds are formed including compounds of formula (IV) and their salts which are used in pharmaceutical and veterinary compositions.
    • 8. 发明专利
    • New method for n-cyclopropylation of aromatic amines, as well as compounds and compositions obtained
    • AU7236494A
    • 1995-02-13
    • AU7236494
    • 1994-07-12
    • SOMFAI EVA
    • SOMFAI EVA
    • C07C227/08C07D215/56C07D215/36A61K31/495
    • Process for the introduction of a cyclopropyl group into a primary or secondary aromatic amine or into heterocyclic compounds containing a secondary nitrogen atom reacting to the corresponding amines or their salts so as to form the corresponding N-cyclopropyl-(1'-carboxy)-derivatives either with the reagent of general formula (I), optionally in the presence of an acid binding agent or with 2,4-dihalogen-butyric acid ester or with chloroacetic acid ester, whereupon the resulting N-(alkoxy-carbonyl)-methyl-derivative is treated with alkali alkylate and dihalogen-ethane to convert the alkoxy-carbonyl-methyl group into a carbalkoxy-cyclopropyl group and subsequently optionally hydrolysing the ester groups if present and optionally eliminating the 1'-carboxyl group introduced in the course of the first step, whereby the last step is carried out optionally after introducing other substituents into the aromatic ring or after eliminating other substituents from the aromatic group. The method is suitable to synthesize 1-cyclopropyl-7-piperazine-1,4-dihydro-quinolone-3-carboxylic acid derivatives. New biologically active compounds are formed including compounds of formula (IV) and their salts which are used in pharmaceutical and veterinary compositions.