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Acid-promoted iron-catalysed dehydrogenative [4 + 2] cycloaddition for the synthesis of quinolines under air

机译:酸促进的铁催化脱氢[4 + 2]环加成反应,在空气中合成喹啉

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An acid-promoted iron-catalysed dehydrogenative [4 + 2] cycloaddition reaction was developed for the synthesis of quinolines using air as a terminal oxidant. Acetic acid was the best cocatalyst for the cycloaddition of N -alkyl anilines with alkenes or alkynes under air. Various quinoline derivatives were obtained in satisfactory-to-excellent yields, and no other byproducts besides water were produced in the reaction. The zebrafish model has become an important vertebrate model for evaluating drug effects. We tested the activity of 3n in zebrafish. The test results showed that 1 μg mL ~(?1) 3n treatments resulted in morphological malformation, and 0.01–0.1 μg mL ~(?1) 3n treatments led to potent angiogenic defects in zebrafish embryos. The results of this study will be of great significance for promoting drug research in cardiovascular and cerebrovascular diseases.
机译:开发了一种酸促进铁催化的脱氢[4 + 2]环加成反应,用于使用空气作为末端氧化剂来合成喹啉。乙酸是在空气中将N-烷基苯胺与烯烃或炔烃环加成的最佳助催化剂。以令人满意的至优异的产率获得了各种喹啉衍生物,并且在反应中除了水之外没有产生其他副产物。斑马鱼模型已成为评估药物作用的重要脊椎动物模型。我们测试了斑马鱼中3n的活性。测试结果表明,1μgmL〜(?1)3n处理导致形态畸形,而0.01–0.1μgmL〜(?1)3n处理导致斑马鱼胚胎中潜在的血管生成缺陷。该研究结果对促进心脑血管疾病的药物研究具有重要意义。

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