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

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.