本文报道了一系列5-取代苯氧基-8-氨基喹啉类化合物(I)的合成和抗疟活性,对其中的一种即5-对氟苯氧基伯喹的实验性疗效和毒性与伯喹作了比较。作者对合成此类化合物的关键中间体5-溴-6-甲氧基-8-硝基喹啉的合成步骤作了改进,减少反应溴量1/2～1/3、增加了中和除溴操作和改用甲苯作重结晶溶剂。另外采用稀硫酸洗涤法除去缩合成品中存在的小量游离8-氨基喹啉,防止了直接成盐可能夹入的杂质。 This paper reports the synthesis and anti-malarial activities of a series of 5-substituted phenoxy-8-aminoquinolines (I), one of which is the experimental efficacy and toxicity of 5-p- Compared with primary quinine. The synthesis of 5-bromo-6-methoxy-8-nitroquinoline, which is the key intermediate for the synthesis of these compounds, has been improved, reducing the amount of reaction bromine by 1/2 ~ 1/3 and adding neutralization Bromine operation and use of toluene as recrystallization solvent. In addition, a small amount of free 8-aminoquinoline present in the condensation product is removed by a dilute sulfuric acid scrubbing process to prevent impurities that may directly form salts.