新型噻吩[2,3- d]嘧啶4(3H) 1衍生物的合成、理化性质及镇痛评价

Dinesh P Kawade, D. Chaple, P. Khedekar
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引用次数: 1

摘要

以不同的脂肪酸为原料,在常规加热和微波辐照下,催化POCl3高效一步无溶剂合成了2-氨基-4,5-取代噻吩-3-碳腈的新型噻吩[2,3-d]嘧啶-4(3H)- 1衍生物。通过元素分析和FTIR、1HNMR和质谱等光谱技术证实了化合物的形成。所有合成的化合物都用Eddy ' s热板法进行了镇痛活性筛选。合成的化合物2d、2k和2h具有良好的镇痛活性,化合物2a、2b、2g和2i具有中等的镇痛活性,其余化合物与标准曲马多相比具有较低的镇痛活性。关键词:POCl3, Thieno[2,3-d]嘧啶-4 (3H)- 1,镇痛活性,涡流热板
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Synthesis, physicochemical characterization and analgesic evaluation of some new thieno [2,3-D] Pyrimidin 4(3H) one derivatives
A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2,3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under both conventional heating and microwave irradiation techniques. The formation of compounds was confirmed via elemental analysis and spectroscopic techniques like FTIR, 1HNMR and mass spectroscopy. All synthesized compounds have been screened for their analgesic activity by using Eddy´s hot plate method. The synthesized compounds 2d, 2k and 2h showed good analgesic activity and compounds 2a, 2b, 2g and 2i showed moderate whereas remaining compounds possessed less analgesic activity compared with standard, Tramadol. Keywords: POCl3, Thieno[2,3-d]pyrimidin-4 (3H)-one, Analgesic activity, Eddy´s hot plate.
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