阿克他利的合成  

Study on the Synthesis of Actarit

作　　者：张雪[1] 李胜辉[1] 王书香[1] 李记太[1] 

机构地区：[1]河北大学化学与环境科学学院,河北保定071002

出　　处：《河北大学学报（自然科学版）》2008年第2期178-181,共4页Journal of Hebei University(Natural Science Edition)

基　　金：河北省自然科学基金资助项目(2006000969;B2007000152)

摘　　要：以苯乙腈为原料,经硝化、水解、还原以及酰化等4步反应对阿克他利（Actarit,对乙酰氨基苯乙酸）及其中间体的合成条件进行了研究和改进.目的产物用元素分析、红外光谱及核磁共振氢谱进行了表征.研究发现对硝基苯乙腈合成的最适温度为7～8℃.在回流温度152℃,对硝基苯乙腈水解且搅拌充分的情况下效果最为理想,对硝基苯乙酸的还原以水溶液中醋酸活化的铁粉为还原剂效果较好.乙酸酐与对氨基苯乙酸的比例为1.5∶1（物质的量比）时对乙酰氨基苯乙酸的合成较好,4步反应总收率可达50.5%.The title compound was prepared from phenylacetonitrile by nitration, hydrolysis, reduction, and acylation. The structure was determined by elemental analysis, IR and ^1H NMR spectra. The optimal conditions were indicated as follows： the appropriate temperature for the preparation of 4-nitrobenzyl cyanide was 7- 8 ℃, the optimal temperature for hydrolysis of 4-nitrobenzyl cyanide was 152℃, 4-nitrophenylacetic acid was reduced in water with Fe powder which was activated by acetic acid and the optimal ratio of acetic anhydride to 4- aminophenylacetic acid was 1.5 ： 1. The overall yield reached 50.5 % under the above conditions. Key words：rheumatoid arthritis; actarit; nitration; hydrolysis; reduction; acylation

关 键 词：类风湿性关节炎 阿克他利 硝化 水解 还原 酰化 

分 类 号：TQ031.2[化学工程]