引用本文:
Zheng Bao ZHAO, Jing GUO, Yuan Gui WEI, Tong Da LIANG. Synthesis of 4-Aminosalicylglycine[J]. Chinese Chemical Letters,
2005, 16(7): 889-892.
Citation: Zheng Bao ZHAO, Jing GUO, Yuan Gui WEI, Tong Da LIANG. Synthesis of 4-Aminosalicylglycine[J]. Chinese Chemical Letters, 2005, 16(7): 889-892.
Citation: Zheng Bao ZHAO, Jing GUO, Yuan Gui WEI, Tong Da LIANG. Synthesis of 4-Aminosalicylglycine[J]. Chinese Chemical Letters, 2005, 16(7): 889-892.
Synthesis of 4-Aminosalicylglycine
摘要:
To search for a better prodrug of 4-aminosalicylic acid that is expected to deliver stably parent drug to colon against the inflammatory bowel disease, a novel 4-aminosalicylic acid derivative was designed and synthesized from 4-aminosalicylic acid. 4-Aminosalicylglycine was prepared from 4-aminosalicylic acid by protecting amino and hydroxyl groups with benzyloxycarbonyl and acetyl, respectively, then the carboxylic acid was converted to acyl chloride which was treated with glycine. After removing the protection groups, 4-aminosalicylglycine was obtained. All the compounds were characterized by FT-IR, 1H-NMR, 13C-NMR spectra. In vivo experiment on rats suggested that the curative effect of 4-aminosalicylglycine was more effective than that of 4-aminosalicylic acid.
English
Synthesis of 4-Aminosalicylglycine
Abstract:
To search for a better prodrug of 4-aminosalicylic acid that is expected to deliver stably parent drug to colon against the inflammatory bowel disease, a novel 4-aminosalicylic acid derivative was designed and synthesized from 4-aminosalicylic acid. 4-Aminosalicylglycine was prepared from 4-aminosalicylic acid by protecting amino and hydroxyl groups with benzyloxycarbonyl and acetyl, respectively, then the carboxylic acid was converted to acyl chloride which was treated with glycine. After removing the protection groups, 4-aminosalicylglycine was obtained. All the compounds were characterized by FT-IR, 1H-NMR, 13C-NMR spectra. In vivo experiment on rats suggested that the curative effect of 4-aminosalicylglycine was more effective than that of 4-aminosalicylic acid.
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Key words:
- 4-Aminosalicylio acid
- / 4-aminosalicylglycine
- / inflammatory bowel disease
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