含硼異腈化合物之合成(Ⅲ):根據文獻報導，目前已知上百種含有異腈官能基(Isocyanide)之天然物。而這些特殊的天然物在抗菌或抗腫瘤上多具顯著的特效。因此，異腈化合物之合成實為一值得深入研究主題。本研究成功藉由Ugi多組成反應合成出含硼之甲醯胺，接著將之脫水轉換為含硼之異腈化合物。 Synthesis of Boron-containing Peptidyl Analogs (Ⅰ):In this research, we have designed and synthesized two series of boron-containing analogs.These compounds could be easily synthesized and purified via simple synthetic operations. In addition, boronic acid and its corresponding boron functional groups are successfully synthesized with mild conditions.
Synthesis of Boron-containing Analogs via Ugi Reaction (Ⅱ):In this research, an Ugi four-component reaction (Ugi-4CR) utilizing formylphenylboronic acids or formylphenylboronate esters under mild condition is developed. The described reactions were accelerated by employing microwave irradiation.In addition, the liquid-liquid acid/base extraction protocol for the purification and isolation of all reported final products were also included making this strategy suitable for the preparation of chemical libraries and provided a unique opportunity to access a broad range of boron-containing analogs.
Synthesis of Boron-containing Isocyanide (Ⅲ):Isocyanide (or isonitrile) is a unique class of functional groups that appears in many biological active natural products. Many of these isocyanide-based natural products can be used as anti-bacterial or anti-tumor agents. It is thus a valuable target functional group in medicinal chemistry.In this research, I have successfully synthesized 4 boron-containing formamides by microwave assisted Ugi-4CR and have good yields. At the same time, I have successfully converted 2 boron-containing formamides to boron-containing isocyanides.