摘要
目的开发一条适合产业化的3-氯-4-(3-氟苄氧基)苯胺的合成工艺路线。方法以间氟氯苄和2-氯-4-硝基苯酚为原料,依次经碳酸钾存在下的缩合反应、铁粉/氯化铵还原得到3-氯-4-(3-氟苄氧基)苯胺。结果总收率为82%。所得产物经TLC、熔点和核磁共振氢谱表征,具有高纯度。结论本方法原料价廉易得,操作简便,环境污染更小,预期适合工业化生产。
OBJECTIVE To develop a practical process for 3-chloro-4-（3-fluorobenzyloxy）aniline. METHODS 3-Chloro- 4-（3-fluorobenzyloxy）aniline was synthesized from 1-（chloromethyl）-3-fluorobenzene and 2-chloro-4-nitrophenol via condensation in the presence of potassium carbonate, followed by reduction with Fe/NH4Cl. RESULTS The overall yield of this process was 82%. The target product was characterized by TLC, melting point and 1H-NMR. CONCLUSION This synthetic process features are cheap and readily available starting materials, robustness, less waste burden, thus should be amenable to industrial production.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2011年第3期245-246,共2页
Chinese Journal of Modern Applied Pharmacy
基金
国家"重大新药创制"科技重大专项(2009ZX09301-007)
上海市基础研究重点项目(09JC1413200)
