利用Ugi反應合成多重含硼化合物(III):本實驗利用Ugi-4CR反應，以簡易的合成與純化方法，成功的合成出一系列含多重硼化合物。實驗結果發現，若起始物含有拉電子基團(F)，則反應需以60oC進行。如含推電子基團(OMe)則需以65oC進行。而不含推或拉電子基團的起始物則只需以50oC即可進行反應。目前正進行生物活性之評估，期望此類化合物能成為新一代BNCT的藥物。 Synthesis of Potassium Peptidyl Trifluoroborates and their Analogs (I):In this research, we have designed and synthesized two series of boron-containing analogues. These compounds could be easily synthesized and purified via simple synthetic operations. Synthesis of Boron-containing Amines by Modified Gabriel Synthesis (II):In this project, we have discovered the optimal synthetic conditions for the synthesis of boron-containing primary amines. Further, we have successfully demonstrated the utilization of these boron-containing primary amine building blocks to generate series of boron-containing Ugi analogues in moderate to good yield. Synthesis of Multiple Boron-containing Analogs via Ugi Reaction (III):In this project, we have successfully synthesized series of multiple boron-containing Ugi analogs. The synthetic methods we have developed provide a simple and efficient protocol to generate series of novel compounds. We’ve found that, if the starting material contains an electron-withdrawing group (EWG) (i.e. -F), the reaction temperature requires to be 60oC. On the other hand, when the electron-donating group (EDG) (i.e. -OMe) is present, a higher reaction temperature (65oC) is required. Interestingly, when neither EDG nor EWG is present, only moderate heating condition (50oC) is necessary. The synthesized boron agents are currently being evaluated for their potential in BNCT application. The result will be reported in due course.
