抗生素重要片段侧链酸的高效合成工艺  

Efficient Synthesis of Antibiotic Side Chain Acid

作　　者：翟丽娟 何丽丽 纪静雯 孙健 Zhai Lijuan;He Lili;Ji Jingwen;Sun Jian(Institute of Agricultural Resources and Environment,Ningxia Academy of Agriculture and Forestry Sciences,Yinchuan,Ningxia 750002)

机构地区：[1]宁夏农林科学院农业资源与环境研究所,宁夏银川750002

出　　处：《宁夏农林科技》2024年第2期18-21,31,共5页Journal of Ningxia Agriculture and Forestry Science and Technology

基　　金：宁夏回族自治区自然科学基金项目(2022AAC03452)。

摘　　要：单环β-内酰胺类抗生素是抗生素新药研发的重要热点领域,在氨基噻唑的C5位引入甲基为重要技术方案之一。在原有合成路线基础上,通过反应机理深度分析,以3-氧戊酸乙酯为起始原料,经5步反应,高效合成了C5位引入甲基的氨基噻唑侧链酸,为候选药物目标化合物DPI-2016的临床前期研究奠定了基础。Monocyclicβ-lactam antibiotics are an important hotspot in the research and development of new antibiotics,and the introduction of methyl at C5 position of aminothiazole is an important solution.In this paper,based on the original synthesis route,through in-depth analysis of the reaction mechanism,the methylated aminothiazole side chain acid at C5 was efficiently synthesized from 3-oxoethylpentanoate as the starting material through five steps of reaction in high efficient way,which laid the foundation of the preclinical research for the candidate drug target compound DPI-2016.

关 键 词：单环β-内酰胺类抗生素 氨基噻唑侧链酸 氨曲南 

分 类 号：TQ465[化学工程—制药化工]