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Highly Efficient Synthesis of 1,4-Dihydropyridine DerivativesUsing DBU

机译:高效合成1,4-二氢吡啶衍生物DBU

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The 1,4-dihydropyridine family is a significant class of pharmacophore compoundsfrequently found in the field of drug such as hypertension and angina treatment.In addition,it is known that these compounds exhibit various activities such as antioxidative,antidiabetic,and antitumor.1 To date,numerous synthetic methods for 1,4-dihydropyridinederivatives have been reported due to such a significant biological importance.For example,Yan's group reported unsymmetric polysubstituted dihydropyridines were synthesized by afour-components reaction of aromatic aldehydes,malononitrile,arylamines,andacetylenedicarboxylate in the presence of triethylamine as a base promoter at roomtemperature.2 However,in the synthesis of the skeleton with β-enaminoimides as asubstrate,heating conditions using piperidine as a base were required.3
机译:1,4-二氢吡啶家族是一类大量药效线化合物,在药物如高血压和心绞痛治疗中发现。另外,这些化合物表现出各种活性,如抗氧化,抗糖尿病和抗肿瘤。迄今为止,由于这种显着的生物重要性,已经报道了许多用于1,4-二氢吡啶的合成方法。例如,由于芳香族醛,丙二腈,芳基胺,苯乙酸二羧酸亚乙酸二乙酰化羧酸甲酯的AFOUR-组分,通过AFOUS-组分的反应合成了许多合成的1,4-二氢吡啶的二氢吡啶。然而,在室温间的三乙胺作为碱启动子。然而,在用β-烯丙基酰亚胺的骨架合成中,需要使用哌啶作为碱的加热条件。

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