稳定同位素标记物D3-左氧氟沙星的合成及表征  

Synthesis and Characterization of Stabilized Isotope D3-Levofloxacin

作　　者：韩涛 赵紫羽 杜诗曼 奉强 张琦 张小玲 HAN Tao;ZHAO Zi-yu;DU Shi-man;FENG Qiang;ZHANG Qi;ZHANG Xiao-ling(Institute of Functional Molecules, College of Chemistry and Life Science, Chengclu Normal University, Chengdu 611130, China)

机构地区：[1]成都师范学院化学与生命科学学院功能分子研究所

出　　处：《化学试剂》2018年第6期589-592,共4页Chemical Reagents

基　　金：四川省教育厅一般资助项目(2018-18ZB0101);四川省教育厅科研创新团队资助项目(2017-17TD0005)

摘　　要：以市售的左氧氟沙星羧酸为原料,以氘代甲醇为稳定同位素标记物前体,经无水哌嗪取代、双氘代甲基化、氢氧化钠水解合成出稳定同位素标记的D3-左氧氟沙星,3步反应总收率为45.5%。目标产物经MS、^1HNMR表征确认,通过高效液相色谱确认化学纯度〉98%,经计算同位素丰度为97.7%。该合成路线具有操作简便、试剂廉价等优点。Stabilized isotope-labeled D3-levofloxacin was synthesized by using commercially available levofloxacin carboxylic acid as starting material and deuterated methanol as a stable isotope-labeled precursor with three steps.The steps are in order of replacing with anhydrous piperazine,bis-deuterated methylation and hydrolized by sodium hydroxide with totally yield of 45. 5%. The target product was confirmed by MS,^1HNMR and HPLC. The chemical purity was higher than 98% and the isotope abundance was 97. 7% by calculation.Designed synthetic route is simple and commercial.

关 键 词：同位素标记 D3-左氧氟沙星 氘代甲基化 

分 类 号：TQ421.6[化学工程] R914.5[医药卫生—药物化学]