本論文主要是研究利用銅試劑來催化合成異吲哚基[1,2-b]喹唑-12（10H）-酮(isoindolo[1,2-b]quinazolin-12(10H)-one)及其衍生物的反應。此反應所合成的產物乃是特別針對具有潛力的藥物Batracylin中的結構進行改良。有關Batracylin的性質，目前從細胞實驗以及動物的實驗結果已發現它可以抑制腫瘤細胞的生成。而其抑制方式是讓細胞的DNA受損而導致無法進一步的進行細胞分裂，最終造成細胞死亡。然而另一個副作用則為N-乙酰化(N-acetylation)的反應常會造成正常細胞的中毒，最終甚至導致老鼠死亡，因此，我們希望能將Batracylin的部份結構進行改良，希望能減少其生物毒性，最終能變成具潛力的藥物。

The contents of this thesis divided into two parts. The first part describes the introduction of isoindolo[1,2-b]quinazolin-12(10H)-one derivatives pharmacological importance, previous reported procedures for the synthesis of these derivatives. Along with these introduction of copper catalyzed tandem cyclizations included in this chapter. Next, aim of the thesis also described as in last part of this chapter.
The second chapter deals about the synthesis of isoindolo[1,2-b]quinazolin-12(10H)-one derivatives by copper catalyzed tandem cyclization from the reaction of 2-iodo(N-(2-bromobenzyl)benzamide substrates and copper cyanide. A wide variety of 2-iodo(N-(2-bromobenzyl)benzamide substrates were utilized for the construction of variety of isoindolo[1,2-b]quinazolin-12(10H)-one derivatives in moderate to excellent yields. Further using the procedure, we synthesized Batracylin drug. Batracylin can inhibit the formation of tumor cells.

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