摘要
磷酸西格列汀传统合成方法存在反应步骤繁琐、生产成本较高及依赖昂贵催化剂等问题。鉴于此,通过优化生物酶催化技术,开发出一种更加经济、环保、操作简便的磷酸西格列汀合成方法:以2,4,5-三氟乙酸为起始原料,以转氨酶为催化剂获得手性胺结构,经过四步反应获得产品,纯度99.9%,总收率67.8%,明显高于已有文献水平。该合成路线为磷酸西格列汀的工业化生产提供了理论支持和实践指导。
Traditional synthesis methods of siegliptin phosphate have problems such as complicated reaction steps,high production cost and de-pendence on expensive catalysts.In view of this,through the optimization of enzyme catalysis technology,a more economical,environmentally friend-ly,easy operation of sitagliptin phosphate synthesis method was developed:With 2,4,5-trifluoroacetic acid as the starting material,with transaminase as catalyst to obtain chiral amine structure,after four steps reaction,the products purity of 99.9%,total yield 67.8%,significantly higher than the existing literature level.This synthetic route provides theoretical support and practical guidance for the industrial production of sitagliptin phosphate.
作者
贾淑红
刘晓斐
占晓广
姬松涛
孙秀伟
韩涛
李月明
Jia Shuhong;Liu Xiaofei;Zhan Xiaoguang;Ji Songtao;Sun Xiuwei;Han Tao;Li Yueming(Jinan Aisi Pharmaceutical Technology Co.,Ltd.,Shandong,250101;Nankai University,Tianjin,300071;Luoyang Desheng Biotechnology Co.,Ltd.,Henan,470800)
出处
《当代化工研究》
2025年第9期167-169,共3页
Modern Chemical Research
基金
山东省科技型中小企业创新能力提升工程项目“磷酸西格列汀创新工艺技术的研发与产业化”(项目编号:2023TSGC0256)。
关键词
磷酸西格列汀
合成
生物酶催化
绿色化学
sitagliptin phosphate
synthesis
biocatalysis
green chemistry
