Synthesis of 4-Aminosalicylglycine

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.

作 者： Zheng Bao ZHAO JING GUO Yuan Gui WEI Tong Da LIANG   作者單位： College of Pharmacy, Shanxi Medical University, Taiyuan 030001  刊 名： 中國化學快報（英文版）  ISTIC SCI 英文刊名： CHINESE CHEMICAL LETTERS  年，卷(期)： 2005 16(7)  分類號： O6  關鍵詞： 4-Aminosalicylio acid   4-aminosalicylglycine   inflammatory bowel disease