The Synthesis of Bioactive Natural Products as a Driving Force for Discovery in Organic Chemistry

生物活性天然产物的合成作为有机化学发现的驱动力

• 批准号: 10596203
• 负责人: BRIAN M STOLTZ
• 金额: $ 58.6万
• 依托单位: CALIFORNIA INSTITUTE OF TECHNOLOGY
• 依托单位国家: 美国
• 财政年份: 2022
• 资助国家: 美国
• 起止时间: 2022-04-01 至 2027-03-31
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10596203
• 关键词: Acylation; Alkylation; Applications Grants; Biological; Carbon; Chemicals; Chemistry; Complex; Development; Elements; Government; Human; Hydrogenation; Industrialization; Investigation; Laboratories; Medicine; Methodology; Methods; Natural Products; Organic Chemistry; Preparation; Process; Public Health; Reaction; Research; Route; Science; Structure; Synthesis Chemistry; Technology; Testing; Transition Elements; arm; bioactive natural products; driving force; new technology; novel; programs; tool

Project Summary/Abstract: The objective of this research program is to discover and develop new reaction methodology en route to the synthesis of complex bioactive molecules. Our proposed studies will focus on the investigation and optimization of technologies that enable the synthesis of core structural and stereochemical subunits prevalent in many bioactive, polycyclic natural products. The processes that we develop will find utility in the synthesis of a wide variety of structures for which there are currently no efficient synthetic roadmaps. Importantly, the methods presented in this application will be useful outside of the contexts described herein and will arm practitioners of synthetic chemistry (in academic, government, and industrial laboratories) with a new set of important tools to access enantioenriched and functionally diverse chemical building blocks for synthesis. The research proposed in this grant application is focused on a) the development of new stereoselective reactions that produce densely substituted building blocks for synthesis, b) the development of transition metal catalyzed reactions for asymmetric alkylation, acylation, and hydrogenation processes, c) the development of these novel methods specifically for the preparation of building blocks containing all-carbon quaternary stereocenters and arrays of stereocenters, and d) the implementation of these new tactics in the syntheses of highly complex, bioactive natural products. These molecules are not only important from a biological standpoint, they also serve as a testing ground for our new technologies. As a consequence of this approach, we will have access to a) novel, medicinally relevant structures, b) a general platform for their synthesis, and c) new synthetic methodology that will impact a host of diverse applications.

项目总结/文摘: