艾拉莫德(T-614)的合成工艺研究  

The Study of the Synthesis of Iguratimod(T-614)

作　　者：丁磊[1] 李小敏[1] 殷晓进[1] 刘立平 尤启冬[3] 

机构地区：[1]江苏先声药物研究有限公司,南京210042 [2]海南先声药业有限公司,海口570314 [3]中国药科大学药学院,南京210009

出　　处：《江苏药学与临床研究》2006年第3期162-164,共3页Jiangsu Pharmacertical and Clinical Research

基　　金：2005年度国家高技术研究发展计划(863计划)引导项目;编号2005AA1250

摘　　要：目的对新药艾拉莫德(1)的合成工艺进行研究。方法以4-氯-3-硝基苯甲醚为起始原料,与苯酚反应生成4-苯氧基-3-硝基苯甲醚,再经还原、甲磺酰化、付-克酰基化、甲酰化、水解、环合,共7步反应制备得到(1)。结果(1)的化学结构经核磁共振谱、质谱确证,纯度(HPLC法)>99%。结论该合成路线较短,反应条件温和,操作简便,收率较高(38%),易于工业化生产。AIM To run a study to the synthesis of the new drug：iguratimod（1）. METHODS 4-chloro-3-nitroanisole, as the starting material, was reacted with phenol to obtain 4-phenoxy-3-nitroanisole, which was successively carried out reductiun、methylsulfonylation、 Friedel-Crafts formylation、hydrolyzafion and cyclization reactions. The compound iguratimod was finally synthesized after the total 7 steps with a high field of 38%, RESULTS The target compound was synthesized successfully and its chemical structure was confirmed by ^1H NMR and ESI-MS. CONCLUSION This procedure has the advantages such as shorter steps, milder reaction conditions and relatively simple operations, it is easily to be manufactured.

关 键 词：艾拉莫德 合成 工艺研究 

分 类 号：TQ463[化学工程—制药化工]