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

    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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