N-取代-5-羟基-1H 吲哚-3-羧酸酯类衍生物的合成  

Synthesis of derivatives of N-alkyl-5-hydroxy-1H-indole-3-carboxylic ester hydrochloride

作　　者：宋艳玲[1] 赵燕芳[2] 宫平[2] 

机构地区：[1]沈阳化工学院制药工程教研室,沈阳110142 [2]沈阳药科大学制药工程学院,沈阳110016

出　　处：《中国新药杂志》2004年第4期335-337,共3页Chinese Journal of New Drugs

摘　　要：目的:以阿比朵尔为先导化合物,设计并合成-系列4-取代胺甲基-5-羟基-1-烃基-2-苯硫基甲基-1H吲哚-3-羧酸乙酯盐酸盐。方法:以4-氯代乙酰乙酸乙酯为起始原料通过硫代、胺化、Nenitzescu反应、Mannich反应、成盐反应共5步反应制得目标产物。由薄层色谱(TLC)确定每步反应终点。结果:目标化合物结构经红外光谱、核磁共振光谱及质谱确证。结论:通过该合成方法合成了9个未见报道的新化合物。Objective: To synthesize some derivatives of N-alkyl-5-hydroxy-lH-indole-3-car-boxylic ester hydrochloride using arbidol as leading compound. Methods: Using 4-chloroethyl acetoac-tate as starting material, the target compounds were synthesized through 5 unite reactions, including sulfurizing,amination,Nenitzescu reaction, Mannich reaction and salt formation. The end up of reaction was determined by TLC. Results: The chemical structure of these target compounds were confirmed by IR,1H-NMR and MS. Conclusion: 9 unreported derivatives of N-alkyl-5-hydroxy-1H-in-dole-3-carboxylic ester hydrochloride were synthesized by this way.

关 键 词：阿比朵尔 N-取代-5-羟基-1H吲哚-3-羧酸酯类衍生物 药物合成 

分 类 号：R914.5[医药卫生—药物化学]