High-throughput photocapture approach for reaction discovery

High-throughput photocapture approach for reaction discovery
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DOI:
10.1073/pnas.2003347117
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发表时间:
2020-06-16
影响因子:
11.1
通讯作者:
Scheidt, Karl A.
Scheidt, Karl A.
中科院分区:
综合性期刊1区
文献类型:
--
作者:
Bayly, Alison A.;McDonald, Benjamin R.;Scheidt, Karl A.

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现代有机反应的发现和发展依赖于大量假设驱动实验的快速评估。反应分析的时间密集性为这种支持新生物活性剂开发的迭代过程的执行提出了最大的实际障碍。为了解决这一关键瓶颈,我们在此报告了一种高通量分析(HTA)反应混合物的方法,通过在384点重氮嘧啶端自组装单层上进行光捕获,并将自组装单层用于基质辅助激光解吸/电离质谱(SAMDI-MS)分析。该分析平台已应用于鉴定单电子促进的酰基唑类还原偶联。
Modern organic reaction discovery and development relies on the rapid assessment of large arrays of hypothesis-driven experiments. The time-intensive nature of reaction analysis presents the greatest practical barrier for the execution of this iterative process that underpins the development of new bioactive agents. Toward addressing this critical bottleneck, we report herein a high-throughput analysis (HTA) method of reaction mixtures by photocapture on a 384-spot diazirine-terminated self-assembled monolayer, and self-assembled monolayers for matrix-assisted laser desorption/ionization mass spectrometry (SAMDI-MS) analysis. This analytical platform has been applied to the identification of a single-electron-promoted reductive coupling of acyl azolium species.