氨磷汀合成方法研究进展

Research Progress in Synthesis of Amifostine

氨磷汀化学名称为2-(3-氨基丙胺基)乙硫醇磷酸酯,主要用于在各种癌症放疗或化疗中的辅助治疗。本文综述了国内外有关氨磷汀化学合成方法工艺路线研究进展和成果,其中主要工艺路线是N-(羟乙基)-1,3-丙二胺经过成盐/卤化反应制备得到N-(2-卤代乙基)-1,3-丙二胺双氢卤酸盐,随后与硫代磷酸化试剂反应制备获得氨磷汀,重点介绍了各工艺的优缺点及其改进。

The chemical name of Amifostine is 2-(3-aminopropylamino)ethylsulfanyl phosphonic acid and mainly used for adjuvant therapy in various cancer radiotherapy or chemotherapy.This paper reviewed the research progress and results of the process route of the chemical synthesis method of amifostine.The main process route was N-(hydroxyethyl)-1,3-propanediamine through salt formation/halogenation reaction to obtain N-(2-haloethyl)-1,3-propanediamine dihydrohalide,then reacted with phosphorothioate reagent to prepare amifostine,focusing on the advantages and disadvantages of these process and its improvements.