首页> 外国专利> N-(5-ACETYL-2-FLUOROPHENYL)-N-METHYLACETAMIDE, METHOD OF PRODUCING N-5-(3-DIMETHYLAMINO-ACRYLOYL)-2-FLUOROPHENYL-N-METHYLACETAMIDE AND METHOD OF PRODUCING N-{2-FLUORO-5-3-THIOPHENE-2-CARBONYL-PYRAZOLO1,5-aPYRIMIDIN-7-YLPHENYL}-N-METHYLACETAMIDE

N-(5-ACETYL-2-FLUOROPHENYL)-N-METHYLACETAMIDE, METHOD OF PRODUCING N-5-(3-DIMETHYLAMINO-ACRYLOYL)-2-FLUOROPHENYL-N-METHYLACETAMIDE AND METHOD OF PRODUCING N-{2-FLUORO-5-3-THIOPHENE-2-CARBONYL-PYRAZOLO1,5-aPYRIMIDIN-7-YLPHENYL}-N-METHYLACETAMIDE

机译：N-（5-乙酰基-2-氟苯甲酰基）-N-甲基乙酰胺，制备N- [5-（3-二甲基氨基-丙烯酰基）-2-氟苯甲酰基] -N-甲基乙酰胺的方法和制备N- {2-氟甲酰胺的方法-5- [3-噻吩-2-羰基-吡唑并[1,5-a]嘧啶-7-YL]苯}}-N-甲基乙酰胺

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摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a method of producing N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methylacetamide of formula (I). The method is realised by reacting N-(5-acetyl-2-fluorophenyl)-N-methylacetamide of formula (VI) with excess N,N-dimethylformamide dimethylacetal (NNDMF-DMA) in the presence of a nonpolar solvent at temperature of 70-90°C. The invention discloses a method of producing a N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methylacetamide compound of formula (II), which involves methylation of N-(5-acetyl-2-fluorophenyl)-acetamide at temperature of 15-50°C, reacting the obtained compound of formula (VI) with NNDMF-DMA, and reacting the obtained compound of formula (I) with (5-amino-1H-pyrazol-4-yl)thiophen-2-yl-methanone in glacial acetic acid at temperature of 60-90°C in the presence of an aliphatic alcohol. The invention also relates to an intermediate compound of formula (VI).;EFFECT: improved method of producing a compound which is an intermediate compound in synthesis of compounds with affinity for the GABA_A receptor.

机译：技术领域本发明涉及一种制备式为<图像文件=“ 00000026.GIF” he =“ 55的N- [5-（3-二甲基氨基-丙烯酰基）-2-氟苯基] -N-甲基乙酰胺的方法“ imgContent =” undefined“ imgFormat =” GIF“ wi =” 37“ />（I）。该方法通过使式为<图像文件=“ 00000027.GIF” he =“ 46” imgContent =“ undefined” imgFormat =“ GIF” wi =“的N-（5-乙酰基-2-氟苯基）-N-甲基乙酰胺反应来实现在非极性溶剂存在下，在70-90°C的温度下，用过量的N，N-二甲基甲酰胺二甲基乙缩醛（NNDMF-DMA）制备38“ />（VI）。本发明公开了一种N- {2-氟-5- [3-（噻吩）-2-羰基-吡唑并[1，5-a]嘧啶-7-基]苯基} -N-甲基乙酰胺化合物的制备方法。公式（II），其中涉及N-（5-乙酰基-2-氟苯基）的甲基化乙酰胺在15-50°C的温度下反应，使所得的式（VI）化合物与NNDMF-DMA反应，并使所得的式（I）化合物与（5-氨基-1H-吡唑-4-基）冰醋酸中的噻吩-2-基-甲酮，在60-90°C的温度下，脂肪族醇存在。本发明还涉及式（VI）的中间体化合物。效果：制备化合物的改进方法，该化合物是在对GABA _{A 受体具有亲和力的化合物的合成中作为中间体化合物。}

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公开/公告号RU2503655C2

专利类型
公开/公告日2014-01-10

原文格式PDF
申请/专利权人 INTERKIM S.A.;
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申请/专利号RU20110133958
发明设计人 MARKILJAS FRANSISKO (ES);SALJARES ROSEL KHUAN (ES);
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申请日2010-01-11
分类号C07C231/12;C07C233/33;C07C233/43;C07D487/04;
国家 RU
入库时间 2022-08-21 15:38:47

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