兰索拉唑有关物质的合成  

Synthesis of the impurities of lansoprazole

作　　者：王毅峰[1] 王庆河[1] 马文希 李瑞娟[1] 程卯生[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中国药物化学杂志》2015年第2期122-124,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的为加强质子泵抑制剂兰索拉唑原料药的质量控制,合成兰索拉唑的相关物质。方法以2-氯甲基-3-甲基-4-(2,2,2-三氟乙氧基)吡啶盐酸盐和2-巯基苯并咪唑为起始原料,用化学法合成了兰索拉唑3个有关物质:2-[[3-甲基-4-(2,2,2-三氟乙氧基)-2-吡啶基]甲基硫代]-1H-苯并咪唑(1)、2-[[3-甲基-4-(2,2,2-三氟乙氧基)-2-吡啶基]甲磺酰基]-1H-苯并咪唑(2)、2-[[3-甲基-1-氧-4-(2,2,2-三氟乙氧基)-2-吡啶基]甲基亚磺酰基]-1H-苯并咪唑(3)。结果与结论目标化合物的结构经质谱、核磁和红外光谱确证,可作为兰索拉唑原料药质量控制的有关物质对照品。所用方法原料易得、反应条件温和、操作简单。Lansoprazole is a new generation of proton pump inhibitor drugs. To improve the quality control of lansoprazole, three impurities （1,2,3） were synthesized. The target compounds were obtained from 2- chloromethyl-3-methyl-4-（2,2, 2-trifluoroethoxy ） pyridine hydrochloride and 2-mercaptobenzimidazole. Their structures were confirmed by MS, IR, 1H-NMR and 13 C-NMR. The three impurities can be used as related substances in the quality control of lansorpozale. It was easy to obtain the raw materials and the reaction conditions were mild.

关 键 词：兰索拉唑 有关物质 合成 

分 类 号：R914.5[医药卫生—药物化学]