磷苯妥英钠的合成工艺  

Synthesis Process of Sodium Phosphophenytoin

作　　者：王廷圣 文敖 WANG Tingsheng;WEN Ao(Guang'an Kingday Pharma&Chem Co.,Ltd.,Guang'an 638400,China)

机构地区：[1]广安凯特制药有限公司,四川广安638400

出　　处：《合成化学》2025年第2期135-139,共5页Chinese Journal of Synthetic Chemistry

摘　　要：磷苯妥英钠是用于抗癫痫或心律失常的药物,注射用磷苯妥英钠解决了癫痫病人在发作时无法口服的问题。本文设计了一种高效一锅法合成磷苯妥英钠的合成工艺。以苯妥英为起始原料,经羟甲基化得到3-羟甲基-苯妥英,该中间体与三氯氧磷和1,2,4-三氮唑在碱性条件下反应,随后向反应液中直接加碱成盐得到磷苯妥英钠(3)。该工艺具有操作步骤简单、原料价廉易得、收率高、产品纯度高和成本低等优势,且无需钯碳氢化,安全环保,尤其适于工业化生产。Fosphenytoin sodium is employed as an antiepileptic or cardiac arrhythmia medication.Injectable fosphenytoin sodium provides a solution for epileptic patients who are unable to ingest it orally during seizures.This paper presents an efficient one-pot synthetic process for the synthesis of fosphenytoin sodium.Phenytoin was employed as the initial reactant,and 3-hydroxymethyl-phenytoin was generated through hydroxymethylation.This intermediate was then subjected to a reaction with trichlormethoxyphosphate and 1,2,4-triazole under alkaline conditions.Subsequently,the direct addition of alkali to the reaction solution was conducted to facilitate the formation of a salt,resulting in the synthesis of phosphophenytoin sodium.The process has the following advantages:simple operation steps,inexpensive and easily obtainable raw materials,high yield,high purity and low cost of the product,and no requirement for palladium hydrocarbon hydrogenation.It is safe and environmentally friendly,and is especially suitable for industrial production.

关 键 词：磷苯妥英钠 抗癫痫或心律失常药 苯妥英钠 一锅法 三氮唑 

分 类 号：TQ463[化学工程—制药化工]