To explore the better prodrug of 4-aminosalicylic acid（4-ASA）with higher activity and less side effects against the inflammatory bowel disease.4-ASA,after a succession of synthesis process,was conjugated with variou...To explore the better prodrug of 4-aminosalicylic acid（4-ASA）with higher activity and less side effects against the inflammatory bowel disease.4-ASA,after a succession of synthesis process,was conjugated with various carder molecules to get seven azo derivatives of 4-ASA.All compounds were characterized by FT-IR,^1H NMR,^13C NMR spectras in detail.New derivatives of 4-ASA were definituded.展开更多
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, r...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, (1)H NMR, (13)C NMR spectra in details. New derivatives of 4-ASA were characterized. The synthetic route was reasonable and feasible.展开更多
文摘To explore the better prodrug of 4-aminosalicylic acid（4-ASA）with higher activity and less side effects against the inflammatory bowel disease.4-ASA,after a succession of synthesis process,was conjugated with various carder molecules to get seven azo derivatives of 4-ASA.All compounds were characterized by FT-IR,^1H NMR,^13C NMR spectras in detail.New derivatives of 4-ASA were definituded.
文摘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, (1)H NMR, (13)C NMR spectra in details. New derivatives of 4-ASA were characterized. The synthetic route was reasonable and feasible.
