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

生物活性天然产物的全合成和有用物质的创造。

基本信息

批准号：
14205128
负责人：
TATSUTA Kuniaki
金额：
$ 33.61万
依托单位：
Waseda University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (A)
财政年份：
2002
资助国家：
日本
起止时间：
2002 至 2004
项目状态：
已结题

项目摘要

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.

龙田集团在2002年至2005年的3年时间里，首次完成了9种具有生物活性的天然产物的全合成和结构鉴定。这些第一次全合成特别需要创造原始的合成概念和方法，包括生物活性天然产物的绝对结构的定义以及其生物活性的验证。我们的主要研究成果包括：1）首次全合成抗生素和雌激素拮抗剂萘放射霉素，开创了新的合成策略; 2）首次全合成抗癌药物UCE 6，应用我们开发的四环素合成方法; 3）分离和鉴定了角化控制物质，具有新的1，3-二氧戊环-4-酮环的碧翠素A和B; 4）首次全合成了抗生素和免疫抑制剂产品，确定了发光菌素A和B的绝对结构; 5）首次全合成了抗癌药和抗HIV药，鞣花酸开发了新的糖基化方法; 6）首次全合成了抗癌药，耳蜗霉素开发了形成10元环的新策略; 7）抗生素的合成研究，Tetrodecamycin的立体异构体的合成; 8）抗癌免疫抑制剂lymphostin的第一个全合成，提示了生物合成过程; 9）抗癌剂BE-542348 B的第一个全合成，确定了绝对结构。