Carbonyl Alkylative Amination as a Tool for the Array Synthesis of Complex Amines

羰基烷基化胺化作为复杂胺阵列合成的工具

• 批准号: 2468412
• 金额: --
• 依托单位: University of Cambridge
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2020
• 资助国家: 英国
• 起止时间: 2020 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2468412
• 关键词: Carbonyl; Alkylative; Amination; Tool; Array

Year 1: Generic training activities for all first-year student members of the CDT.Year 2-4: Microscale array synthesis allows for the systematic interrogation of chemical interactions with minimal material use. The zinc-mediated carbonyl alkylative amination reaction's multicomponent nature and generality makes it ideal for generating diverse libraries of complex amines. We will develop a platform for the high throughput-enabled generation of microscale complex amine arrays. Microscale reaction conditions and product generation have been confirmed but issues with reactive species prevent simple LCMS analysis. Instead, parallel scavenger-resin based purification allows for reaction outcome analysis by NMR. A new workflow based on immediate reaction purification coupled with high throughput NMR is proposed, with the CAA reactivity on microscale confirmed. However, a reaction material mass loss issue currently prevents further optimisation and development.

第一年：CDT所有一年级学生成员的通用培训活动。第二年至第四年：微型阵列合成允许以最少的材料使用系统地询问化学相互作用。锌介导的羰基烷基化胺化反应的多组分性质和一般性使其成为生成各种复合胺文库的理想选择。我们将为高通量生成微尺度复合胺阵列开发一个平台。已经确定了微尺度的反应条件和产物生成，但活性物种的问题阻碍了简单的LC MS分析。取而代之的是，基于平行清除剂树脂的纯化允许通过核磁共振来分析反应结果。提出了一种基于即时反应纯化和高通量核磁共振的新流程，并在微尺度上证实了CAA的反应性。然而，反应材料的质量损失问题目前阻碍了进一步的优化和发展。