S-(+)-布洛芬衍生物的合成  

Synthesis of ibuprofen derivatives

作　　者：宋恒[1] 黄彬[1] 敖桂珍[1] 刘金宜[1] 莫凌萱[1] 

机构地区：[1]苏州大学药学院药物化学教研室,江苏苏州215123

出　　处：《化学试剂》2013年第7期653-654,669,共3页Chemical Reagents

基　　金：江苏高校优势学科建设工程项目

摘　　要：一些非甾体抗炎药可减少阿尔茨海默症脑内老年斑的形成和炎症,但其长期服用会产生严重的胃肠道副作用。将S-(+)-布洛芬与L-氨基酸连接,设计了一系列布洛芬衍生物。以S-(+)-布洛芬为原料,与草酰氯反应生成酰氯,再与L-氨基酸反应,共合成了5个标题化合物,其结构均经1HNMR、IR和HR-MS确证。Some nonsteroidal anti-inflammatory drugs （NSAIDs） can reduce inflammation and formation of senile plaque in brains of Alzheimer＇s disease. However, long-term use of NSAIDs will lead to serious gastrointestinal side effects. A series of S-（ ＋ ）-ibuprofen derivatives were de- signed by coupling S-（ ＋ ）-ibuprofen with L-amino acids through amino acid-specific carrier-mediated transport sys- tem. Target compounds were synthesized from ibuprofen by acyl chloride reaction with oxalyl chloride and condensation reaction with L-amino acid, and their structures were con- firmed by I HNMR,IR and HR-MS.

关 键 词：S-(+)-布洛芬衍生物 合成 阿尔茨海默症 

分 类 号：O625.5[理学—有机化学]