Enantioselective Ammonium Enolate Based Michael-Henry and Michael-Henry-Aldol Cascade Reactions: Development, Mechanistic Insight, and Applications for Morphine Family Analgesics

基于迈克尔-亨利和迈克尔-亨利-羟醛级联反应的对映选择性烯醇铵：吗啡系列镇痛药的开发、机理洞察和应用

• 批准号: 509064606
• 负责人: Professor Dr. Thomas Nugent
• 金额: --
• 依托单位: Department of Life Sciences and Chemistry
• 依托单位国家: 德国
• 项目类别: Research Grants
• 资助国家: 德国
• 项目状态: 未结题
• 来源: https://gepris.dfg.de/gepris/projekt/509064606?language=en
• 关键词: Enantioselective; Ammonium; Enolate; Based; Michael

Given the significance of medicine to society, the efficient synthesis of molecules of medicinal relevance has always been a vital goal within academic granting agencies. To reach that goal, synthetic design principles are coupled with insightful strategy, and their execution exposes students to the learning outcomes required to face the next generation of more advanced challenges. Without these types of projects, some pharmaceutical drugs would simply not be discovered or discovered but never brought to market for the treatment of disease. In this context, the study of morphine analogs continues unabated to this day and has motivated us to contribute a highly step-efficient new synthetic strategy for the synthesis of morphine. A successful project outcome would allow the findings to be applied to the synthesis of previously inaccessible morphine analogs for medicinal chemistry exploration as drug candidates.

鉴于医学对社会的重要性，有效合成具有医学相关性的分子一直是学术资助机构的一个重要目标。为了实现这一目标，综合设计原则与富有洞察力的策略相结合，其执行使学生能够获得面对下一代更高级挑战所需的学习成果。如果没有这些类型的项目，一些药物根本不会被发现或被发现但永远不会被推向市场用于治疗疾病。在此背景下，对吗啡类似物的研究至今仍未减弱，并激励我们为吗啡的合成贡献一种高效的新合成策略。成功的项目成果将使研究结果能够应用于合成以前无法获得的吗啡类似物，用于作为候选药物的药物化学探索。