中文摘要
本项目拟开展具有独特、复杂化学结构和重要生理活性的若干不同类型海洋天然产物的全合成研究。通过项目的实施，完成了Salinosporamide-A及其类似物和Nakadomarin A的仿生不对称全合成；首次完成结构复杂的海洋天然产物communesin F的全合成；我们对所取得的阶段性成果及时进行应用，成功完成了具有重要生理活性的吲哚生物碱vincorine、minfiesine和ardeemin的全合成；同时，跟踪本学科领域的最新研究成果，首次完成了疫霉菌性激素α1的不对称全合成及其绝对立体化学的确定，揭示了一个70多年的科学疑案；实现了lophotoxin关键合成中间体的合成；并实现了桉烷倍半萜(-)-1α,14-dihydroxy-5,10-bisepieudesma-4(15), 11(13)-diene的首次不对称全合成。上述研究成果共发表相关论文22篇，申请专利4项，得到了国际同行的广泛关注和认可。
英文摘要
We have achieved practically the projected goals toward the selected target total synthesis of several structurally unique and biologically significant marine natural products, which include: (1) design, strategic development, and biomimetic asymmetric total syntheses of (-)-salinosporamide A (NPI-0052) and nakadomarin A; (2) design, strategic development, and first total synthesis of communesin F, a characteristic polycyclic marine indole alkaloid; and (3) strategic applications in the efficient total syntheses of several other indole alkaloids including vincorine, minifiesine, and (-)-ardeemin. In addition, one of our PI (Y. Qin) and his team achieved the first asymmetric synthesis and stereostructural determination of the ?1 hormone. Strategic development towards the total synthesis of marine diterpenoid lophotoxin led to the construction of an advanced model ring skeleton intermediate and an effective general asymmetric total synthesis of eudesmane sesquiterpenoids. Part of the above research results have been published (22 publications) in peer-reviewed journals and 4 patents, which have received world-wide attention and appreciation from the community of synthetic organic chemistry of natural products.
结题摘要
本项目拟开展具有独特、复杂化学结构和重要生理活性的若干不同类型海洋天然产物的全合成研究。通过项目的实施，完成了Salinosporamide-A及其类似物和Nakadomarin A的仿生不对称全合成；首次完成结构复杂的海洋天然产物communesin F的全合成；我们对所取得的阶段性成果及时进行应用，成功完成了具有重要生理活性的吲哚生物碱vincorine、minfiesine和ardeemin的全合成；同时，跟踪本学科领域的最新研究成果，首次完成了疫霉菌性激素α1的不对称全合成及其绝对立体化学的确定，揭示了一个70多年的科学疑案；实现了lophotoxin关键合成中间体的合成；并实现了桉烷倍半萜(-)-1α,14-dihydroxy-5,10-bisepieudesma-4(15), 11(13)-diene的首次不对称全合成。上述研究成果共发表相关论文22篇，申请专利4项，得到了国际同行的广泛关注和认可。