一鍋化及超音波輔助合成含硫、硒元素之有生物活性雜環小分子和牛樟芝菌絲體萃取物之衍生物的合成

Abstract

摘要 在化學的有機合成中，利用超音波來合成藥物是非常少見的，而本篇論文主要是利用超音波、一鍋化來輔助合成2-iminothiazoles、2-iminoselenazoles、ketosulfides這三種具有生物活性的雜環分子。其結果非常成功，具有非常好的產率。而且很幸運的，我們還得到2-iminoselenazoles的中間體X-ray的繞射圖 (化合物56) 由這個發現我們可以推測它的生成反應機制。而在合成2-iminothiazoles的時候，我們也得到X-ray的繞射圖 (化合物 31d) 發現我們合成出來的產物結構並非一些報導中所認為的imidazole-2-thiones，而是2-iminothiazoles。在另外一個部分，牛樟芝的萃取衍生物合成方面，也發現一些具有抑制蛋白質5-lipoxygenase生物活性的結構。在這些牛樟芝衍生物的化合物合成的中，我們意外發現如果用勞森試劑(Lawesson's reagent)來和編號10的衍生物反應，會將2-methylpent-2-ene切除。這是一個之前沒有人報導過的一個實驗。

In organic synthetic chemistry, the use of ultrasound to synthetic drugs are very rare, and this paper is the use of ultrasound, to assist the synthesis of a pot of 2-iminothiazoles, 2-iminoselenazoles, ketosulfides three biologically active hetero ring molecules. The result was very successful, with very good yields. And very lucky, we also get 2-iminoselenazoles intermediate X-ray diffraction diagram (Compound 56) From this we can surmise that it was found to generate response mechanisms. In the synthesis of 2-iminothiazoles when we get X-ray diffraction diagram (compound 31d) found out we synthesized some reports in the product structure is not thought imidazole-2-thiones, but 2-iminothiazoles. In another section, the extraction of Antrodia synthesis of derivatives, also found that some 5-lipoxygenase inhibiting the biological activity of the protein structure. These synthetic compounds Antrodia derivatives in, we accidentally discovered derivative if Lawesson's reagent and number 10, will be 2-methylpent-2-ene removed. This is a before nobody had reported an experiment.