GOALI: C-H Bond Activation and Functionalization Methods for Medicinal and Process Chemistry

GOALI：药物和过程化学的 C-H 键激活和功能化方法

• 批准号: 1012883
• 负责人: Robert Maleczka
• 金额: $ 48.4万
• 依托单位: Michigan State University
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-10-01 至 2014-09-30
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1012883&HistoricalAwards=false
• 关键词: GOALI; Bond; Activation; Functionalization; Methods

This GOALI project will continue work to establish Ir-catalyzed C-H borylations as an efficient route to aryl and heteroaryl boronic esters and allied molecules. While boronic esters serve as useful building blocks for pharmaceuticals, materials, and other valuable compounds, their preparation often requires the employment of haolgenated aromatics. This reliance on halogenated starting materials raises environmental concerns and limits the availability of many potentially useful boronic esters. Studies aimed at developing new and orthogonal strategies for the direct borylation and further functionalization of pharmaceutically relevant molecules will be undertaken. Screening of diverse substrates and catalysts/reagent combinations will be used to develop mechanistic models of these reactions and to expand the chemical space in which these reactions can operate. With this award, the Chemical Synthesis Program is supporting the research of Professors Robert E. Maleczka, Jr. and Milton R. Smith, III of the Department of Chemistry at Michigan State University, who will be working in collaboration with Dr. Yongkui Sun of Merck and in consultation with the American Chemical Society-Green Chemistry Institute's Pharmaceutical Roundtable. Professor Smith and Maleczka's collaborative research efforts revolve around the development of green chemistry methods for the formation and subsequent reaction of C-B bonds. Successful development of these reactions will positively impact discovery and process development in the pharmaceutical and other high tech industries. In addition, the academic research groups at Michigan State University will be exposed to the technical problems of concern at a major pharmaceutical company.

这个GOALI项目将继续致力于建立Ir催化的C-H硼化反应作为芳基和杂芳基硼酸酯和相关分子的有效途径。 虽然硼酸酯用作药物、材料和其它有价值化合物的有用结构单元，但它们的制备通常需要使用卤代芳族化合物。 这种对卤化起始材料的依赖引起了环境问题，并限制了许多潜在有用的硼酸酯的可用性。 将开展旨在开发新的正交策略的研究，用于药物相关分子的直接硼基化和进一步功能化。 筛选不同的底物和催化剂/试剂组合将用于开发这些反应的机理模型，并扩大这些反应可以操作的化学空间。 有了这个奖项，化学合成计划是支持教授罗伯特E。小马莱茨卡和米尔顿R.密歇根州立大学化学系的史密斯三世，他将与默克公司的孙永奎博士合作，并与美国化学会-绿色化学研究所的制药圆桌会议协商。 史密斯教授和Maleczka的合作研究工作围绕着绿色化学方法的形成和随后的C-B键反应的发展。 这些反应的成功开发将对制药和其他高科技行业的发现和工艺开发产生积极影响。 此外，密歇根州立大学的学术研究小组将接触到一家大型制药公司关注的技术问题。