4-氨基水杨酸不饱和脂肪酸类衍生物的合成(英文)  

Synthesis of unsaturated fatty acid derivatives of 4-aminosalicylic acid

作　　者：姜爱雯[1] 赵正保[1] 

机构地区：[1]山西医科大学药学院,山西太原030001

出　　处：《中国医药导报》2010年第9期37-38,118,共3页China Medical Herald

摘　　要：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。Objective： To explore the better prodrug of 4-aminosalicylic acid with higher activity and less side effects against 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.

关 键 词：4-氨基水杨酸 4-氨基水杨酸不饱和脂肪酸衍生物 炎性肠病 

分 类 号：R914.5[医药卫生—药物化学]