Synthesis of azo derivatives of 4-aminosalicylic acid

Zheng Bao Zhao Hui Xia Zheng Yuan Gui Wei Jiang Liu

引用本文: Zheng Bao Zhao,  Hui Xia Zheng,  Yuan Gui Wei,  Jiang Liu. Synthesis of azo derivatives of 4-aminosalicylic acid[J]. Chinese Chemical Letters, 2007, 18(6): 639-642. doi: 10.1016/j.cclet.2007.04.031 shu
Citation:  Zheng Bao Zhao,  Hui Xia Zheng,  Yuan Gui Wei,  Jiang Liu. Synthesis of azo derivatives of 4-aminosalicylic acid[J]. Chinese Chemical Letters, 2007, 18(6): 639-642. doi: 10.1016/j.cclet.2007.04.031 shu

Synthesis of azo derivatives of 4-aminosalicylic acid

摘要: For searching a better 4-aminosalicylic acid derivative with higher activity and less side effects against the inflammatory bowel disease, 4-aminosalicylic acid (4-ASA) was protected by benzyloxycarbonyl and acetyl, respectively.The resultant was hydrogenized to remove protective group of amino group, then the product was reacted with NaNO2 to give diazonium salt, which was conjugated with salicylic acid, hydroxybenzene, N-salicyloyl glycine acid to get azo derivatives of 4-ASA.The azo derivatives were hydrolyzed under the alkaline condition to get the target products.All compounds were characterized by FT-IR, 1H NMR, 13C NMR spectra in details.New derivatives of 4-ASA were characterized.The synthetic route was reasonable and feasible.

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  • 收稿日期:  2007-02-26
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