Development of Synthetic Methods toward Biologically Active Compou

为了合成多种C-核苷，我们打算将D-核糖基和D-脱氧核糖基与含氮芳香杂环化合物进行联合收割机结合。以二苯基硒二酰氧基化物、二酰氧基碘代苯、四（三甲基硅基）硅烷和硫代异羟肟酸酯（巴顿试剂）为自由基试剂，在光化学和热化学条件下进行了研究，结果表明，巴顿反应可用于C-核苷的合成。因此，通过使用巴顿反应合成了几种C-核苷。接下来，利用离子反应合成了C-核苷：将典型的芳香杂环锂盐引入苄基保护的D-核糖上，然后进行酸环化反应。

In order to synthesize many kinds of C-nucleosides, we intended to combine D-ribosyl and D-deoxyribosyl radicals with N-containing aromatic heterocycles. As the radical reagents, diphenylselenium diacyloxylate, (diacyloxyiodo)benzene, tetrakis(trimethylsilyl)silane, and thiohydroxamic acid ester known as the Barton reagent were examined under photochemical and thermal conditions.The result showed that the Barton reaction could be applicable for the C-nucleoside synthesis. Therefore several C-nucleosides were synthesized by employing the Barton reaction. The other reagents required the further investigation for the C-nucleoside synthesis.Next, the synthesis of C-nucleosides was performed by utilizing the ionic reaction : the lithium salt of typical aromatic heterocycles was introduced onto the benzyl-protected D-ribose followed by the acid-cyclization.