4-氨基水杨酸不饱和脂肪酸类衍生物的合成

目的：为了探索更好的且具有较高的活性和对炎症性肠病毒副作用少的4-氨基水杨酸前药。方法：首先以4-ASA为原料依次用氯甲酸苄酯和乙酸酐分别保护氨基和酚羟基,然后再氢化还原脱去氨基上的保护基,合成的新化合物经MS、IR、1H-NMR、13C-NMR确证。结果：本实验合成了3个4-氨基水杨酸与不饱和脂肪酸形成的酰胺类化合物。结论：该合成路线是合理和可行的。

Synthesis of unsaturated fatty acid derivatives of 4-aminosalicylic acid

Objective: To explore the better prodrug of 4-aminosalicylic acid with higher activity and less side effects a-gainst the inflammatory bowel disease. Methods: First of all, methods to 4-ASA for the raw materials followed by formic acid with benzyl chloride and acetic anhydride, respectively, amino and hydroxyl protection. Hydride reduction and then taked off on the amino-protective group, Synthesis of new compounds by IR, MS, 1H-NMR,13C-NMR confirmed. Results: Synthesis of three amide compounds about unsaturated fatty acid of 4-aminosalicylic acid. Conclusion: The synthetic route is reasonable and feasible.