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筆墨輕點(diǎn)新蟲 (初入文壇)
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A green and efficient multicomponent one-pot synthesis of Hantzsch polyhydroquinoline was achieved bythe condensation of aldehydes, dimedone, ethylacetoacetate and ammonium acetate at room temperatureusing environmentally benign modified Montmorillonite supported Ni0-nanoparticles as catalyst. The welldispersed Ni0-nanoparticles having a high surface to volume ratio have promising features for the reactionsuch as easy removal of the catalyst, solvent-free, shorter reaction time, high product yields (about 95%)and easy work up procedure. There is no significant effect of electron withdrawing or donating nature ofsubstituent on aldehydes in the formation of polyhydroquinoline derivatives. 4-Substituted 1,4-dihydropyridine (DHP) nucleus comprises alarge family of medicinally important compounds such as Ca2+chan-nel blockers and some of the representative compounds of this classpossess acaricidal, insecticidal, bactericidal and herbicidal activities[1]. 1,4-Dihydropyridine possesses a variety of biological activities,such as, vasodilator, bronchodilator, anti-atherosclerotic, antitumor,geroprotective, hepatoprotective and antidiabetic agent [2–5]. Photo-catalytic oxidation of these compounds to pyridine derivatives consti-tutes the principal metabolic pathway in biological systems [6].Therefore, oxidative aromatization of DHPs has been a subject ofgreat interest of organic and medicinal chemists. |
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用對(duì)環(huán)境無害的改性蒙脫石支持的Nio納米顆粒作為催化劑在室溫下對(duì)醛類，雙甲酮，乙基乙酰乙酸和乙酸銨進(jìn)行縮合反應(yīng)，實(shí)現(xiàn)用綠色、高效、多組分Hantzsch 多聚羥基喹啉的一鍋合成法。 具有高表面體積比、分散良好的Nio納米顆粒具有適于反應(yīng)的良好特性，如易于除去催化劑，無溶劑的，反應(yīng)時(shí)間更短，產(chǎn)品產(chǎn)率高（約95％）和操作簡(jiǎn)便等。在多聚羥基喹啉衍生物的形成過程中醛取代基沒有明顯的吸電子或供電子作用。 4 - 取代-1,4 - 二氫吡啶（DHP）核包括一個(gè)大家族的重要的藥用化合物，如鈣離子通道阻斷劑和一些具有代表性的具有殺螨，殺蟲，殺菌和除草活性的一類化合物【1】。 1,4 - 二氫吡啶類具有多種生物活性，如，血管擴(kuò)張，支氣管擴(kuò)張，抗動(dòng)脈粥樣硬化，抗腫瘤，抗老化（老化保護(hù)），保肝和抗糖尿病等【2-5】。這些化合物經(jīng)光催化氧化反應(yīng)產(chǎn)生吡啶衍生物在生物系統(tǒng)中構(gòu)成了一主要的代謝途徑【6】。因此，二氫吡啶氧化芳香化一直是有機(jī)和藥物化學(xué)家極大興趣的主題。 |
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