一种盐酸普拉克索片降解杂质BI-II546CL的制备方法  

Synthesis of pramipexole tablets to degrade impurity BI-II546CL

作　　者：刘旭[1] 戴华山 尹利献 梁慧兴[1] 罗宏军 LIU Xu;DAI Hua-shan;YIN Li-xian;LIANG Hui-xing;LUO Hong-jun(Yangtze River Pharmaceutical Group Co.,Ltd.,Taizhou Jiangsu 225321)

机构地区：[1]扬子江药业集团有限公司,江苏泰州225321

出　　处：《中南药学》2022年第10期2318-2320,共3页Central South Pharmacy

摘　　要：目的 建立一种高效的盐酸普拉克索片降解杂质BI-II546CL的制备方法。方法 由7-羟基普拉克索经氨基保护、酰胺化、氧化、水解制得。结果 氧化过程得到了优化,避免产生多种氧化杂质,总收率达到54.7%。结论 合成路线安全、环保、高效,收率得到明显提升。杂质BI-II546CL经液质联用、红外光谱、核磁共振进一步表征确证。Objective To develop a highly effective preparation method for pramipexole hydrochloride tablets to degrade impurity BI-II546CL.Methods The preparation was obtained from 7-hydroxypramipexole by amino protection,amidation,oxidation and hydrolysis.Results The oxidation process was optimized to avoid various oxidation impurities,and the total yield reached 54.7%.Conclusion The synthesis route is safe,environmentally friendly and efficient,and the yield is improved significantly.The structure of impurity BI-II546CL is further confirmed by LC-MS,IR and NMR.

关 键 词：BI-II546CL 普拉克索 降解杂质 合成 

分 类 号：TQ463.53[化学工程—制药化工]