吡罗昔康-d_3的合成  

Synthesis of Piroxicam-d_3

作　　者：梁大伟[1] 张漫 谭琳 王悦秋[1] LIANG Da-wei;ZHANG Man;TAN Lin;WANG Yue-qiu(Department of Pharmacy & Medical Laboratory,Ya’an Polytechnic College,Ya’an 625000,China)

机构地区：[1]雅安职业技术学院药学与检验系,四川雅安625000

出　　处：《食品与药品》2019年第2期120-123,共4页Food and Drug

基　　金：雅安市应用技术研究与开发项目(2017YYJSKF15)

摘　　要：目的开发稳定同位素氘代标记吡罗昔康-d_3的合成方法。方法以邻苯甲酰磺酰亚胺为原料,氘代碘甲烷为氘代标记试剂,经过烷基化、重排、氘代甲基化与酯的氨解得到氘代标记的吡罗昔康-d_3。结果总收率为26.6%,化学纯度为99.2%,氘代丰度为99.3%,目标化合物结构经质谱、核磁共振等表征确定。结论该4步合成路线方法简单,原料易得、反应条件易于控制,产品可用于其在药代动力学方面的研究。Objective To develop a method of the synthesis of the deuterium-labeled piroxicam-d3.Methods Piroxicam-d3 was synthesized from saccharin via alkylation,rearrangement,deuterated methylation and ammoniation.Deuterated methyl iodide was used as the labeling reagent.Results The total yield was 26.6%,and the structure of the target compound was confirmed by MS and NMR.Its chemical purity was 99.2%and the deuterated abundance was 99.3%.Conclusion The four-step syntheses can be simple and efficient,and all starting materials used in this study can be commercially available.It can be used as an internal standard for pharmacological studies.

关 键 词：氘代标记 吡罗昔康 合成 

分 类 号：R914.5[医药卫生—药物化学]