【摘要】：阿戈美拉汀是一種褪黑激素的萘類衍生物,化學(xué)名為N-[2-(7-甲氧基-1-萘基)乙基]乙酰胺。阿戈美拉汀基本對(duì)所有類型的抑郁癥均有較好的治療效果,且副作用較少,是更有前景的抗抑郁藥物。而控制藥物的純度,是保證藥物安全有效的重要前提,保證雜質(zhì)的含量是控制藥物純度,也是控制藥物安全、有效的重要因素。目前,我們已經(jīng)合成了阿戈美拉汀的四個(gè)有關(guān)物質(zhì)。分別為2-(7-甲氧基-1-萘基)乙胺化合物,2,2,-二(7-甲氧基-1-萘基)二乙胺化合物,2,2,-二(7-甲氧基-1-萘基)二乙酰胺化合物,2-((7-甲氧基-3,4-二氫-1-萘基)乙基)乙酰胺化合物。其中伯胺化合物以7-甲氧基-3,4-二氫-1-萘酮為原料經(jīng)過與氰乙酸加成,DDQ脫氫,再經(jīng)Li Al H4還原生成。仲胺化合物以7-甲氧基-3,4-二氫-1-萘酮為原料經(jīng)過與氰乙酸加成,DDQ脫氫,再經(jīng)雷尼鎳催化氫化反應(yīng)生成。仲胺乙酰胺化合物是在合成仲胺化合物的基礎(chǔ)上經(jīng)過酰胺化反應(yīng)生成。2-((7-甲氧基-3,4-二氫-1-萘基)乙基)乙酰胺化合物以7-甲氧基-3,4-二氫-1-萘酮為原料經(jīng)過與氰乙酸加成,經(jīng)Li Al H4還原,再經(jīng)酰胺化反應(yīng)生成。滔羅定是一種廣譜抗菌藥,臨床上可用于多種感染疾病的治療,其對(duì)臨床應(yīng)用具有重要作用。滔羅定良好的殺菌和抗內(nèi)毒素作用,是因?yàn)槠湓谒芤褐兴鉃樘狭_安、甲醛的性質(zhì)。我們采取兩種方法對(duì)滔羅定水溶液含量進(jìn)行測(cè)定。分別為分光光度計(jì)法、高效液相色譜法。其中分光光度計(jì)法采用變色酸捕獲甲醛,高效液相色譜法采用柱前衍生化手段,分別使用丹磺酰氯,萘磺酰氯將滔羅定水溶液分解的滔羅安片段衍生化,生成可被檢測(cè)的產(chǎn)物,再進(jìn)行含量測(cè)定。
[Abstract]:Agomelatine is a Naphthalene derivative of melatonin, the chemical name is N-[2-(7-methoxyl-1-Naphthyl) ethyl] acetamide. the chemical name is N-[2-(7-methoxy-1-Naphthyl) ethyl] acetamide. Agomelatine is a more promising antidepressant because of its good therapeutic effect on all types of depression and less side effects. Controlling the purity of drugs is an important prerequisite to ensure the safety and effectiveness of drugs. Ensuring the content of impurities is not only an important factor to control the purity of drugs, but also an important factor to control the safety and effectiveness of drugs. At present, we have synthesized four related substances of Agomelatine. 2-(7-methoxy-1-Naphthyl) ethylamine compound, 2, 2, bis (7-methoxy-1-Naphthyl) diethylamine compound, 2, 2,-bis (7-methoxy-1-Naphthyl) diacetamide compound, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2, 2. 2-(7-methoxy-3, 4-dihydro-1-naphthyl) acetamide compound. The primary amine compound was prepared from 7-methoxy-3, 4-dihydro-1-Naphthalene ketone by addition with cyanoacetic acid, dehydrogenase by DDQ, and then reduced by Li Al H4. The secondary amine compound was synthesized from 7-methoxy-3, 4-dihydro-1-Naphthalene ketone by addition with cyanoacetic acid, DDQ dehydrogenation and catalytic hydrogenation of Raney nickel. The secondary amine acetamide compound is formed by amidation on the basis of the synthesis of secondary amine compound. 2-(7-methoxy-3, 4-dihydro-1-naphthyl) acetamide compound with 7-methoxyl-3, 4-bis Hydrogen-1-Naphthalene ketone was added with cyanoacetic acid as raw material. It was reduced by Li Al H 4 and then aminated to form. Torodin is a kind of broad-spectrum antibacterial drug, which can be used in the treatment of many kinds of infectious diseases, and plays an important role in clinical application. Torodin has good bactericidal and anti-endotoxin effects because of its hydrolysis to Toluoan and formaldehyde in aqueous solution. We used two methods to determine the content of Tonodin aqueous solution. They were spectrophotometry and high performance liquid chromatography (HPLC). Among them, formaldehyde was captured by discoloration acid by spectrophotometer, and Danesulfonyl chloride and naphthalene sulfonyl chloride were used to derivatize the surroan fragment decomposed by Danzuloyl chloride and Naphthalene sulfonyl chloride, respectively, to form a product that could be detected. Then the content was determined.
【學(xué)位授予單位】：吉林大學(xué)
【學(xué)位級(jí)別】：碩士
【學(xué)位授予年份】：2017
【分類號(hào)】：R914;R927.2

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