5-氨基-7-氟喹啉的合成

Synthesis of 5-Amino-7-fluoroquinoline

标题化合物是一个具有较强药用价值的医药中间体,具有显著的生理活性和广泛的应用前景,但其合成相关的报道较少且收率低。以简单易得的2-氯-3-氟苯甲酸为起始原料,经取代、霍夫曼降解、关环、硝化、铁粉还原以及加氢脱8-氯6步反应得到标题化合物。该工艺路线成本低、易操作,总收率高达43%,适合工业化生产。

5-Amino-7-fluoroquinoline is a pharmaceutical intermediate with significant medicinal value,significant physiological activity and wide application prospects but the reports on its synthesis are particularly rare with lower yield.The process for the synthesis of 5-amino-7-fluoroquinoline was investigated.The target compound was prepared from 2-chloro-3-fluorobenzoic acid as the starting material via six steps including substitution,Huffman degradation,ring closure,nitration,iron powder reduction and reduction of 8-cdechlorination.The synthetic route was low cost and easy to operate with higher total yield（43%）,and it is suitable for industrial production.