臺灣博碩士論文加值系統

近幾十年來，天然物的雜環結構越來越受到重視，許多的有機化學家紛紛投入此領域中，提出各種雜環化合物的合成研究。由於其抗癌活性，我們對於2-phenyl-4-quinolone的衍生物合成深感興趣。然而此類化合物對水和有機溶劑的溶解度很低，為了解決此溶解度問題，我們設計利用甲醛和不同的2級胺進行Mannich反應，成功的合成出2-phenyl-4-quinolone的衍生物，期望增加其水溶性，以提升其臨床藥物上之應用價值。相關的抗癌活性篩選正在研究中。

Compounds isolated from natural products containing a heterocyclic ring represent an important class of biologically active molecules that are widespread in nature. Organic chemists have reported many methods for the total synthesis of these compounds.
In our laboratory, we are interested in the synthesis of 2-phenyl-4-quinolone derivatives due to their anticancer activity. On the other hand, these derivatives showed the poor solubility in water and organic solvent. In order to solve this problem, we designed to synthesize these derivatives by Mannich reaction using formaldehyde and various secondary amines. We have synthesized 2-phenyl-4-quonolone derivatives successfully. The cytotoxicity of these derivatives are in progress.

英文摘要： Ⅰ
中文摘要： Ⅱ
謝誌： III
第一章：序論
第一節：研究歷史回顧與藥理活性 1
第二節：2-苯基-4-喹啉酮衍生物的合成回顧 5
第三節：研究動機與目的 8
第四節：2-苯基-4-喹啉酮結構與生物活性關係整理 12
第二章：合成方法
第一節：合成策略 14
第二節：結果與討論 16
第三章：實驗結果與討論 27
第四章：實驗部分
第一節：本實驗所使用之儀器與藥品 29
第二節：2-苯基-4-喹啉酮衍生物全合成之實驗步驟 30
第五章：光譜數據 38
參考文獻 53

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