Ohyoshi Takayuki, Mitsugi Keisuke, Higuma Tatsuya, Ichimura Fumitaka, Yoshida Masahito, Kigoshi Hideo
Department of Chemistry, Graduate School of Pure and Applied Sciences, University of Tsukuba 1-1-1 Tennodai Tsukuba 305-8571 Japan
RSC Adv. 2019 Mar 5;9(13):7321-7323. doi: 10.1039/c8ra10346a. eCollection 2019 Mar 1.
We have established a concise and scalable synthetic pathway for phelligridins A (1), C (2) and D (3). The synthetic highlights were Suzuki-Miyaura coupling and aldol-type condensation of α-pyrone. Phelligridin A was synthesized in four steps, while phelligridins C and D were each synthesized in six steps. Furthermore, we have revealed that the whole structure is essential for the cytotoxicity of phelligridins.
我们已经建立了一条简洁且可扩展的合成路线来合成桑黄菌素A（1）、C（2）和D（3）。合成的亮点是铃木-宫浦偶联反应和α-吡喃酮的羟醛型缩合反应。桑黄菌素A通过四步合成，而桑黄菌素C和D各自通过六步合成。此外，我们还揭示了完整结构对于桑黄菌素的细胞毒性至关重要。
