Automated Multistep Continuous Flow Synthesis of 2-(1H-Indol-3-yl)thiazole Derivatives.
Automated Multistep Continuous Flow Synthesis of 2-(1H-Indol-3-yl)thiazole Derivatives.
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2-(1H-吲哚-3-基)噻唑衍生物的自动化多步连续流动合成。
DOI：
10.1055/s-0031-1290953
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发表时间：
2012
期刊：
影响因子：
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通讯作者：
Cosford,NicholasDP
中科院分区：
文献类型：
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作者：
Pagano,Nicholas;Heil,MarinthaL;Cosford,NicholasDP
使用Syrris AFRICA®合成站报道了2-（1h -吲哚-3-基）噻唑的多步连续流组装。顺序的Hantzsch噻唑合成、去酮化和Fischer吲哚合成为高功能化、药理意义显著的2-（1h -吲哚-3-基）噻唑提供了快速有效的途径。这些复杂的类似药物的小分子在不到15分钟的反应时间内产生，收率很高（在不分离中间体的情况下，三个化学步骤可以产生38-82%）。
The multistep continuous flow assembly of 2-(1H-indol-3-yl)thiazoles using a Syrris AFRICA®synthesis station is reported. Sequential Hantzsch thiazole synthesis, deketalization, and Fischer indole synthesis provides rapid and efficient access to highly functionalized, pharmacologically significant 2-(1H-indol-3-yl)thiazoles. These complex drug-like small molecules are generated in reaction times of less than 15 minutes and in high yields (38–82% over three chemical steps without isolation of intermediates).