Green Synthesis of Alzheimer′s Disease Probes Aftobetin and Analogues Enabled by Flow Technology and Heterogeneous Photocatalysis,ChemSusChem

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Green Synthesis of Alzheimer′s Disease Probes Aftobetin and Analogues Enabled by Flow Technology and Heterogeneous Photocatalysis
ChemSusChem ( IF 7.5 ) Pub Date : 2024-07-19 , DOI: 10.1002/cssc.202401214
Yongjiu Li ₁ , Xin Liu ₂ , Qiong Liu ₃ , Yuchen Wang ₂ , Fener Chen ₄ , Chenguang Liu ₅

Affiliation

Flow synthesis and heterogeneous photocatalysis were integrated to develop a fully-flow synthesis protocol of AD probe aftobetin. This process featured the heterogeneous photo-air oxidation replacing toxic chromium oxidation, heterogeneous photo-nickel C−N coupling replacing noble palladium catalysis, a modified esterification to circumvent the difficult-to-remove dicyclohexylurea. Furthermore, C−N coupling, esterification and Knoevenagel condensation were telescoped together to simplify workup and purification.

中文翻译：

阿尔茨海默病探针 Aftobetin 和类似物的绿色合成，通过流动技术和非均相光催化实现

将流动合成和非均相光催化相结合，开发了 AD 探针 aftobetin 的全流合成方案。该工艺的特点是非均相光空气氧化取代了有毒的铬氧化，非均相光镍 C-N 偶联取代了贵金属钯催化，一种改进的酯化反应以规避难以去除的二环己脲。此外，将 C-N 偶联、酯化和 Knoevenagel 缩合一起放大，以简化检查和纯化。

更新日期：2024-07-19

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