Total Syntheses of Bioactive Natural Products and Creation of Useful Substances.

Tatsuta团队从2002年到2005年用3年的时间完成了9种生物活性天然产物的首次全合成和结构鉴定。这些首次的全合成特别需要创造原始的合成概念和方法，包括对生物活性天然产物的绝对结构的定义以及对其生物活性的验证。我们取得的成果如下：1)首次全合成抗生素和雌激素拮抗剂，开创新策略；2)首次应用我们开发的四环素合成方法学全合成抗癌药物UCE6；3)分离和结构鉴定角化控制物质--具有新的1，3-二氧戊环-4-酮环的三叶皂苷A和B；4)首次全合成抗生素和免疫抑制剂产品，确定其绝对结构；5)首次全合成抗癌和抗HIV、鞣花酸，开发新的糖基化方法；6)首次全合成抗癌药物，开发新的10元环形成策略；7)合成研究抗生素，四环素合成立体异构体；8)首次全合成抗癌药物和免疫抑制剂，淋巴蛋白建议生物合成过程；9)首次全合成抗癌药物，BE-542348B确定绝对结构。

The Tatsuta group has completed the first total syntheses and the structural elucidations of 9 bioactive natural products for 3 years from 2002 to 2005. These first total syntheses especially required the creation of original synthesis concepts and methodologies, and included the definition of the absolute structure of the bioactive natural products as well as the verification of their biological activities. Our accomplishments are the following.1)The first total synthesis of antibiotic and estrogen antagonist, napyradiomycin to create the new strategy ; 2)the first total synthesis of anticancer, UCE6 by application of our developed methodology of tetracycline synthesis ; 3)the isolation and structural determination of a keratinization-controlling substances, spilacleosides A and B having a novel 1,3-dioxolan-4-one ring ; 4)the first total synthesis of antibiotic and immunosuppressant products, luminacins A and B to determine their absolute structures ; 5)the first total synthesis of anticancer and anti-HIV, ellagic acids to develop new glycosylation method ; 6)the first total synthesis of anticancer, cochleamycin to develop new strategies for the formation of 10-membered rings ; 7)the synthetic studies on antibiotic, tetrodecamycin to synthesize the stereoisomer ; 8)the first total synthesis of anticancer and immunosuppressant, lymphostin to suggest the biosynthetic process ; 9)the first total synthesis of anticancer, BE-542348B to determine the absolute structure.