由於世界人口的結構日益老化,對於新藥的需求愈來愈高,因此新藥的研發速度就變得很重要。組合式化學(combinatorial chemistry)能快速合成與結合高效能的生物活性測試,目前已成為藥物設計及研發一項有力的工具,為目前新藥研發的主要途徑。 而目前組合式化學合成的核心技術主要是利用固相合成(solid-phase synthesis)的方法來合成分子庫。因為以固相合成為主的組合式化學可在短時間合成大量的化合物且純化方法簡單。在新藥的開發過程中,可以縮短研發時間,減少金錢和人力花費。 目前新藥開發的方向有兩個:一是使用電腦軟體輔助藥物設計,可以有計畫地改變取代基,產生出多樣性不同組合的化合物。一是從天然化合物和酵素中尋找具有藥性的前驅物。本研究藉由此兩種方法利用固相組合式方法來合成2,5-dioxopiperazine及tetrahydro-β-carbolinone之衍生物。 As a result to the population of the world aging, the demand for new medicine is getting more and more. It is very important for the velocity of new medicine research. Therefore, combinatorial chemistry has become a powerful tool by which large numbers of structurally distinct molecules may be synthesized speedily and then be submitted for biological testing. The core technique of combinatorial chemistry is mainly using solid phase synthesis to prepare compound libraries. Combinatorial chemistry by the way of solid phase synthesis can synthesize a lot of compounds in a time and resource-effective manner. There are two main approaches for drug discovery: one utilizes computer programs to design core structures with suitable substituent group and to produce variety of combined compounds. The other seeks active lead structures from natural compounds and enzyme-bound ligands. This study is to synthesize derivatives of 2,5-dioxopiperazine and tetrahydro-β-carbolinone using solid phase synthesis in the above two methods.