普拉洛芬有关物质的合成
Synthesis of Related Substances of Pranoprofen
肖虎 1都建卫 1刘梦瑶 1李帅 1张岱州1
作者信息
- 1. 山东省药学科学院,山东省黏膜与皮肤给药技术重点实验室,山东济南 250101
- 折叠
摘要
为有效控制普拉洛芬(1)原料药的质量,合成了4种有关物质,分别是:2-(5H-[1]苯并吡喃[2,3-b]吡啶-7-基)-丙烯酸(有关物质A)、2-(5-氧代-[1]苯并吡喃[2,3-b]吡啶-7-基)丙酸(有关物质B)、2-羟基-2-(5H-[l]苯并吡喃[2,3-b]吡啶-7-基)丙酸(有关物质C)和2-(5-羟基-[1]苯并吡喃[2,3-b]吡啶-7-基)丙酸(有关物质D),并用1H NMR、13CNMR、MS进行了结构确证.各有关物质的合成路线步骤较短、反应条件温和,产物纯度均达98.5％以上,为1的质量控制提供参考.其中,有关物质A和C的合成为首次报道.
Abstract
In order to effectively control the quality of pranoprofen(1),four related substances were synthesized,namely 2-(5H-chromeno[2,3-b]pyridin-7-yl)acrylic acid(related substance A),2-(5-oxo-5H-chromeno[2,3-b]-pyridin-7-yl)propanoic acid(related substance B),2-hydroxyl-2-(5H-chromeno[2,3-b]pyridin-7-yl)propanoic acid(related substance C),2-(5-hydroxy-5H-chromeno[2,3-b]pyridin-7-yl)propanoic acid(related substance D),and their structures were confirmed by 1H NMR,13C NMR and MS.The synthetic routes of these four related substances were short with mild reaction conditions,and their purities were more than 98.5％,providing some references for the the quality control of 1.Among them,the synthesis routes of related substances A and C were reported at the first time.
关键词
普拉洛芬/非甾体抗炎药/有关物质/合成Key words
pranoprofen/nonsteroidal anti-inflammatory drug/related substance/synthesis引用本文复制引用
出版年
2024
NETL
NSTL
万方数据