我們利用化合物26a - e及化合物28f 與Pd經偶合反應,形成diaryl acetylene,再加入NaN3,利用合成triazole的環化加成反應,開發出以微波消化有效率方式,找出適當的微波溫度與溶媒,合成一系列Combretastatin A-4之1,2,3–三唑類似物 (31a - f),產率為30% ~ 86%,藉由K-562血癌細胞之細胞週期測試,探討其生物活性。
We use the coupling reaction of Pd to form a diaryl acetylene, generated diaryl acetylene, adding NaN3, the use of synthetic triazole ring of addition reaction, developed by microwave digestion method, to establishment appropriate microwave temperature and solvent, synthesis a series of Combretastatin A-4 1,2,3 - triazolo analogues (31a - f ), the yield is 30% to 86%, by cell cycle of human leukemia K-562 tumor cell line to evaluate its biological activity.