一种新型的 PIFA/KOH 促进方法合成 C2-芳酰化苯并噻唑作为潜在的药物支架。
A Novel PIFA/KOH Promoted Approach to Synthesize C2-arylacylated Benzothiazoles as Potential Drug Scaffolds.
机构信息
College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
出版信息
Molecules. 2022 Jan 22;27(3):726. doi: 10.3390/molecules27030726.
To discover an efficient and convenient method to synthesize C2-arylacylated benzothiazoles as potential drug scaffolds, a novel [bis(trifluoroacetoxy)iodo]benzene(PIFA)/KOH synergistically promoted direct ring-opening C2-arylacylation reaction of -benzothiazoles with aryl methyl ketones has been developed. Various substrates were tolerated under optimized conditions affording the C2-arylacylation products in 70-95% yields for 38 examples. A plausible mechanism was also proposed based on a series of controlled experiments.
为了发现一种高效、便捷的方法来合成作为潜在药物支架的 C2-芳基酰化苯并噻唑，我们开发了一种新型[双（三氟乙酰氧基）碘]苯（PIFA）/KOH 协同促进的 -苯并噻唑与芳基甲基酮的直接开环 C2-芳基酰化反应。在优化条件下，各种底物都能耐受，得到 38 个实例中 70-95%的 C2-芳基酰化产物。还基于一系列对照实验提出了一个合理的反应机理。
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