2,4-二氯-6-甲氧基喹啉-7-醇的合成

Synthesis of 2,4-Dichloro-6-methoxyquinoline-7-ol

以5-氨基-2-甲氧基苯酚和丙二酸为原料,在三氯氧磷溶剂中,一步反应合成目标化合物2,4-二氯-6-甲氧基喹啉-7-醇,通过1HNMR、13CNMR和ESI-MS对其结构进行确证,并通过单因素实验对合成条件进行优化。结果表明,在物料比n(丙二酸)∶n(5-氨基-2-甲氧基苯酚)为1.1∶1、反应温度为100℃、反应时间为5 h的最优合成条件下,目标化合物收率达到65.4%。该研究为喹啉类化合物库提供了一种结构新颖并可以继续衍生化的母核分子。

Using 5-amino-2-methoxyphenol and malonic acid as raw materials,phosphoryl trichloride as a solvent,we synthesized the target compound 2,4-dichloro-6-methoxyquinoline-7-ol by a one-step reaction.Moreover,we characterized its structure by 1HNMR,13CNMR,and ESI-MS.Furthermore,we optimized the synthetic conditions by single-factor experiments.The results show the yield of the target compound reaches 65.4%under the optimal conditions as follows:the molar ratio of malonic acid to 5-amino-2-methoxyphenol of 1.1∶1,the reaction temperature of 100℃,and the reaction time of 5 h.This study provides a novel derivated parent nuclear molecule for quinoline library.