Supplement to Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling

在交叉偶联中利用烷基胺和烷基醇的补充

• 批准号: 10436560
• 负责人: Mary P Watson
• 金额: $ 4.82万
• 依托单位: UNIVERSITY OF DELAWARE
• 依托单位国家: 美国
• 财政年份: 2019
• 资助国家: 美国
• 起止时间: 2019-06-01 至 2024-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10436560
• 关键词: Alcohols; Alkenes; Amines; Biology; Chemistry; Chlorides; Coupling; Cyclization; Development; Educational process of instructing; Educational workshop; Future; Goals; Mentors; Periodicity; Reaction; Research; Salts; Series; Training; career networking; experience; graduate student; insight; method development; programs; success

This supplement to R35 GM131816 is focused on the development of a series of new deaminative cross-couplings and the training of graduate student Bria Garcia, in line with the goals of PA-21- 071. The scientific goals of this supplement are to develop (1) reductive cross-electrophile couplings of alkylpyridinium salts and (hetero)aryl chlorides, and (2) cascade cyclizations of alkylpyridinium salts tethered to alkenes to deliver a range of cyclic products. Both these reactions transform readily available starting materials into valuable motifs found in bioactive molecules. This research will hone Ms. Garcia’s expertise in catalytic method development. It will also greatly enhance her research capabilities by giving her experiences in high-throughput experimentation (HTE), collaborative interactions and insight with medicinal chemists at Pfizer, Inc., and proficiency in developing stereoselective transformations. This supplement proposal also includes a mentoring plan, including participation in UD’s Chemistry-Biology Interface program, multiple courses and workshops, teaching and mentoring experience, and professional networking opportunities, to maximize Ms. Garcia’s training and future success.

本R35 GM 131816的补充侧重于开发一系列新的脱氨剂 交叉耦合和研究生布里亚加西亚的培训，符合PA-21的目标， 071.本补充的科学目标是开发（1）还原性交叉亲电试剂 烷基吡啶鎓盐和（杂）芳基氯化物的偶联，和（2）烷基吡啶鎓盐和（杂）芳基氯化物的级联环化， 烷基吡啶鎓盐与烯烃连接以提供一系列环状产物。这两种反应 将容易获得的起始材料转化为生物活性分子中发现的有价值的基序。 这项研究将磨练加西亚女士在催化方法开发方面的专业知识。它也将大大 通过提供她在高通量实验方面的经验来增强她的研究能力 (HTE)，与辉瑞公司的药物化学家进行协作互动和深入了解，和 在发展立体选择性转化的熟练程度。该补充建议还包括 一个指导计划，包括参与UD的化学-生物学界面计划，多个 课程和讲习班、教学和辅导经验以及专业网络 机会，以最大限度地提高加西亚女士的培训和未来的成功。