(I) 酸催化合成苯并咪唑連接吲哚啉衍生物(II) 一鍋化合成具有抗結核菌活性之橢圓玫瑰樹鹼衍生物

Abstract

本論文分為兩部分： 第一部分為開發以苯并咪唑之2號碳上接鄰氨基苄基作為起始物之合成策略，製備苯并咪唑連接吲哚啉衍生物 (functionalized benzimidazole linked indoline)，並將此方法應用於多樣的官能基，由於尚未有苯并咪唑連接吲哚啉衍生物之相關文獻的發表，因此期望能開啟藥物研究的新領域，亦期望此雙雜環分子結構能擁有豐富的生物活性。 第二部分為以高效率之一鍋化反應合成具有抗結核菌能力之橢圓玫瑰樹鹼的衍生物，藉由改變其官能基進行結構與活性之探討，並期望能提升抗菌能力。

This thesis has two parts: The first part is about synthesis of benzimidazole linked indoline derivatives from C-2-linked-o-aminobenzyl benzimidazole by acid catalyst. This method can apply to various funtional groups. There is no published paper refer to benzimidazole linked indoline derivatives, so we hope these heterobicyclic molecules can show more bioactivity and also hope this thesis can open a new page for research of drugs. The second part is about One-pot synthesis of derivative of ellipticine which has the activity against Mycobacterium tuberculosis. We hope we can improve its activity of anti-TB by changing different funtional groups to study the structure–activity relationship.