摘要
6,7,8-三氟-1,4-二氢-4-氧代-3-喹啉羧酸酯(Ⅰ)经氟乙基化,合成药物中间体6,7,8-三氟-1-(2-氟乙基)-1,4-二氢-4-氧代-3-喹啉羧酸酯。实验表明,用1-溴-2-氟乙烷作为氟乙基化试剂的收率高于用对甲苯磺酸氟乙酯作为氟乙基化试剂的收率,当Ⅰ的用量为6.77 g时,用1-溴-2-氟乙烷进行氟乙基化反应的最佳工艺条件为:反应温度120℃,反应时间8 h,K I的用量6 g,1-溴-2-氟乙烷为5 mL,产品收率90%以上。
6,7,8-Trifluoro-（2-fluoroethyl）- 1,4-dihydro-4-oxoquino-line-3-ethylcarbonate was synthesized using 6,7,8-trifluoro-1,4-dihydro-4-oxoquino-3-ethylcarbonate as raw material through the fluoroethylation reaction. Results showed that using BrCH2CH2F as fluoroethylation reagent was better than using TsOCH2CH2F. The optimal reaction conditions of fluoroethylation are that reaction temperature is 120℃, reaction time is 8 h,the amounts of KI is 6 g and the amounts of BrCH2CH2F is 5 mL,the yield is over 90%.
出处
《应用化工》
CAS
CSCD
2008年第8期927-929,共3页
Applied Chemical Industry
关键词
喹啉羧酸酯
氟乙基化反应
合成
ethylearbonate
fluoroethylation reaction
synthesis
