Development of a divergent synthesis of 4- and 5-membered heterocycles and its application to the synthesis of bioactive natural product

杂环化合物被用于制药、农用化学品和功能材料。最近，含氧四元杂环氧杂环氧杂环己烷被报道为一种有用的骨架，可用于提高药物质量。我们开发了一种以磷和氧组成的O，P-缩醛为关键中间体合成氧杂环己烷的简便方法。这种方法的特点是在一次反应中环保地双重使用磷原子。我们还成功地用我们的方法在短步骤内合成了具有抗癌活性的天然产物。

Heterocyclic compounds are utilized in pharmaceuticals, agrochemicals and functional materials. Recently, oxygen-containing 4-membered heterocycles, oxetane, has been reported as a useful skeleton to improve a pharmaceutical quality. We developed a facile oxetane synthesis using O,P-acetal consisted of phosphorous and oxygen as a key intermediate. The feature of this method is eco-conscious double use of phosphorous atom in one reaction. We also succeeded in synthesizing natural product having anticancer activity in short steps using our method.