王其灼, 耿国武, 張在鈞, 董祖兴, 沈仲柟. 抗疟药物的研究 Ⅰ.4-羟基-7-氯喹啉酸制备的改進J. 药学学报, 1963, 10(3): 183-187.
引用本文: 王其灼, 耿国武, 張在鈞, 董祖兴, 沈仲柟. 抗疟药物的研究 Ⅰ.4-羟基-7-氯喹啉酸制备的改進J. 药学学报, 1963, 10(3): 183-187.
shu
WANG CHI-CHO, GENG GUO-U, ZHANG ZAI-GYN, DUNG ZU-XING AND SHEEN JONG-NAN, . STUDIES ON ANTIMALARIALS——I.AN IMPROVED PREPARATION OF 7-CHLORO-4-HYDROXY-3-QUINOLINECARBOXYLIC ACIDJ. Acta Pharmaceutica Sinica, 1963, 10(3): 183-187.
Citation: WANG CHI-CHO, GENG GUO-U, ZHANG ZAI-GYN, DUNG ZU-XING AND SHEEN JONG-NAN, . STUDIES ON ANTIMALARIALS——I.AN IMPROVED PREPARATION OF 7-CHLORO-4-HYDROXY-3-QUINOLINECARBOXYLIC ACIDJ. Acta Pharmaceutica Sinica, 1963, 10(3): 183-187.
shu

抗疟药物的研究 Ⅰ.4-羟基-7-氯喹啉酸制备的改進

STUDIES ON ANTIMALARIALS——I.AN IMPROVED PREPARATION OF 7-CHLORO-4-HYDROXY-3-QUINOLINECARBOXYLIC ACID

    摘要
  • 摘要: 抗疟药氯喹生产的重要中间体——4-羟基-7-氯喹啉酸(Ⅴ),原用的甲脒法,缩合收率很低。经改进,加原甲酸乙酯参与反应,并找到硝酸铵为有效催化剂,控制适当的反应条件,从间氯苯胺至Ⅴ的四步反应,总收卒为75—80%。即单批的收率较原法提高了5倍以上。经推广到生产上,解决了主要技术关键,与现有各生产路线相较,有其独特的先进性。

     

    Abstract: The Price's procedure for the preparation of 7-chloro-4-hydroxy-3-quinolinecar-boxylic acid (V), a key intermediate for chloroquine production, has been modified. Ammonium nitrate has been found as an effective promoter in the reaction of (Ⅰ) to (Ⅱ). Under suitable conditions, the modified method gave 75-80% overall yield of (Ⅴ), against m-chloro aniline. Thus, it makes possible a more economical production of chloroquine and other 4-aminoquinoline antimalarials.

     

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