1.快速利用Fmoc保護之胺及酸合成聚縮胺酸 在有機合成常常會被用到的就是保護基，而Fmoc是胺基的保護基其中的一種。在傳統上，它通常使用piperidine或是morpholine來去保護(deprotection)，但處理起來相當不易。本篇我們使用KF(potassium fluoride)和TEA(triethylamine)溶於DMF的中性條件來將Fmoc去保護，並在同一步驟下(one-pot procedure)，將得到的胺類化合物與酸類化合物使用多種不同的偶合試劑進行偶合反應，來合成聚縮胺酸(ploypeptides)。 2.固相組合式合成Isoquinolone衍生物 在人類生活水準的提高，相對醫療的需求更是日趨重視，因此藥物的發展更形重要。我們發現isoquinolone的衍生物都有人相繼報導它具有藥物活性，它的活性包括了抑制焦慮(anxiolytic)、抗精神病(antipsychotic)、抗關節炎(antiarthritic)及抗心絞痛(antianginal)等藥性，所以我們希望能用固相組合式合成(solid phase combinatorial synthesis)的方法來大量合成這一系列的衍生物，並了接相關結構的活性。我們合成的方法是使用hexamethyl disiloxane、P2O5和POCl3三個試劑將phenylethyl carbamates 合環成isoquinolines. 1.快速利用Fmoc保護之胺及酸合成聚縮胺酸 The use of protecting groups in organic synthesis is very common, and the Fmoc is one of the protecting groups for amine groups. In general, the Fmoc can be deprotected by using piperidine or morpholine, but it is hard to deal with the reaction. Here, we use KF (potassium fluoride) and TFA (triethylamine) with DMF as solvent in a mild condition to cleave Fmoc. Meanwhile, in this one-pot procedure, we couple the desired amines with acid and various coupling reagents to synthesize ploypetides. 2.固相組合式合成Isoquinolone衍生物 Due to the raise of living standard and the highly needs of medical treatment, the development of medicine becomes crucial to us. According to the literature, we have found that the derivatives of isoquinolone show antipsychotic, antiarthritic, antianginal activities, and the inhibition of anxity. Hence, we expect to apply the solid phase combinatiorial synthesis to prepare a series of isoquinolone derivatives in a rapid and plentiful fashion. We use hexamethyl disiloxane, P2O5 and POCl3 as reagents for the cyclization of phenylethyl carbamates to the isoquinolines. At last, we will test the activity of this series of compounds and find out the active site of the relative structures in the future.
