抗生素重要片段侧链酸的高效合成工艺
Efficient Synthesis of Antibiotic Side Chain Acid
翟丽娟 1何丽丽 1纪静雯 1孙健1
作者信息
- 1. 宁夏农林科学院农业资源与环境研究所,宁夏 银川 750002
- 折叠
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.
Abstract
Monocyclic β-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Key words
Monocyclic β-lactam antibiotics/Amino thiazole side chain acid/Aztreonam引用本文复制引用
基金项目
宁夏回族自治区自然科学基金项目(2022AAC03452)
出版年
2024
国家科技期刊平台
NSTL
万方数据