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

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.