微波辐射快速合成喹诺酮类药物关键中间体7-卤代-6-氟-1-甲基-4-氧代-1,4-二氢-[1,3]硫氮杂环丁烷并[3,2-a]喹啉-3-羧酸乙酯(英文)  

Microwave assisted synthesis of ethyl 7-halo-6-fluoro-1-methyl-4-oxo-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate as a key intermediate for tricyclic quinolones

作　　者：宋林晨[1] 王建强[1] 马淑涛[1] 

机构地区：[1]山东大学药学院药物化学研究所,山东济南250012

出　　处：《中国药物化学杂志》2009年第3期214-217,共4页Chinese Journal of Medicinal Chemistry

基　　金：National Natural Science Foundation of China(20872081);Natural Science Foundation of Shandong Province(Y2006C31);Science and Technology Development Project of Shandong Province(2005GG3202098)

摘　　要：采用微波辐射法简便、快速、高效地合成喹诺酮类药物关键中间体7-卤代-6-氟-1-甲基-4-氧代-1,4-二氢-[1,3]硫氮杂环丁烷并[3,2-a]喹啉-3-羧酸乙酯。中间产物及目标化合物的结构经IR、1H-NMR、MS谱和元素分析确证。结果表明在微波辐射下反应物分子内环合反应速度显著加快,中间产物及目标化合物的收率均有所提高。To find a simple ,rapid and efficient method for the synthesis of ethyl 7-halo-6-fluoro-1- methyl-4-oxo-1,4-dihydro-[ 1,3 ] thiazeto [ 3,2-α] quinoline-3-carboxylate under microwave irradiation condition and to improve its synthetic procedure. The structure of this intermediate was confirmed by IR, ^1H-NMR, MS and elemental analysis. The result showed that the use of the microwave irradiation could accelerate the intramolecular cyclization reaction significantly and increase the yield.

关 键 词：微波辐射法 三环喹诺酮 环化 

分 类 号：R914.5[医药卫生—药物化学]