Scalable Total Synthesis of biologically interesting Natural Products via late stage CH-Oxidation

通过后期 CH 氧化可大规模全合成具有生物学意义的天然产物

• 批准号: 263006796
• 负责人: Professor Dr. Konrad Tiefenbacher
• 金额: --
• 依托单位: Department of Chemistry
• 依托单位国家: 德国
• 项目类别: Research Grants
• 财政年份: 2014
• 资助国家: 德国
• 起止时间: 2013-12-31 至 2017-12-31
• 项目状态: 已结题
• 来源: https://gepris.dfg.de/gepris/projekt/263006796?language=en
• 关键词: Scalable; Total; Synthesis; biologically; interesting

The primary goal of the project is the short (10-15 linear steps) and scalable synthesis of the natural products Merrilactone A and Vinigrol. To demonstrate the scalability of the routes, it is planned to synthesize several hundred milligrams of the natural products and a series of derivatives. This should allow the exploration of the promising biological profile and the delineation of first structure-activity relationships. The two natural products will be synthesized in optically active form, which is especially interesting in the case of Vinigrol, since it so far has been accessible only in racemic form.

该项目的主要目标是天然产物 Merrilactone A 和 Vinigrol 的短时间（10-15 个线性步骤）和可扩展合成。为了证明该路线的可扩展性，计划合成数百毫克天然产物和一系列衍生物。这应该可以探索有前景的生物学特征并描绘第一个结构-活性关系。这两种天然产物将以光学活性形式合成，这对于维尼醇来说尤其有趣，因为迄今为止它只能以外消旋形式获得。

项目成果

Synthesis and Neurotrophic Activity Studies of Illicium Sesquiterpene Natural Product Analogues.

• DOI: 10.1002/chem.201605362
• 发表时间: 2017-03
• 期刊: Chemistry
• 作者: Johannes Richers;A. Pöthig;E. Herdtweck;C. Sippel;F. Hausch;K. Tiefenbacher