Synthesis of 7-chloro-6-fluoro-1-(4-fluorophenyl)-4-oxo-1, 4-dihydro-1, 8-naphthyridine-3-carboxylic acid

2018 4th International Conference on Environmental Science and Material Application

生态环境科学;材料科学

Zhang, Jianqing^1 ; Duan, Yongli^1 ; Xiong, Hehua^1 ; Zhuang, Yingmei^1 ; Tang, Qidong^1

School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang

330013, China^1

关键词: Anticancer drug;    Efficient synthesis;    Ms spectrum;    Synthesis method;    Total yield;   

Others  :  https://iopscience.iop.org/article/10.1088/1755-1315/252/2/022087/pdf
DOI  :  10.1088/1755-1315/252/2/022087

来源: IOP

【 摘 要 】

7-chloro-6-fluoro-1-(4-fluorophenyl)-4-oxo-1, 4-dihydro-1, 8-naphthyridine-3-carboxylic acid is an important intermediate for the many biologically active anticancer drugs. In this research, a rapid and efficient synthesis of compounds 7 was established. Compound 7 consisting of methyl (Z)-2-(2, 5-dichloro-6-fluoronicotinoyl)-3-((4-fluorophenyl) (methyl) amino) acrylate was synthesized by two steps including substitution and hydrolysis. The synthesis method was optimized, and structure was confirmed by 1H NMR and MS spectrum. The synthesis method is optimized. The total yield of the two steps is 63.69%.