摘要
以二苯醚与丙酮酸乙酯为原料,经傅克酰基化一步合成恶唑菌酮关键中间体2-(4-苯氧基苯基)乳酸乙酯,考察了溶剂、投料比、AlCl3用量、缚酸剂、温度对收率的影响。-25℃,CH2Cl2为溶剂,NaHCO3为缚酸剂,n(二苯醚)∶n(丙酮酸乙酯)∶n(AlCl3)=1.4∶1.0∶1.2,2-(4-苯氧基苯基)乳酸乙酯收率86.2%,目标产物结构经IR、1 H NMR确证。
Ethyl 2-(4-phenoxyphenyl)lactate is the key intermediate of famoxadone.It can be synthesized by Friedel-Crafts acylation,using diphenyl oxide and ethyl pyruvate as raw materials.The effects of solvent,molar ratio of raw material,acid binding reagent and temperature on the reaction were studied.At-25℃,CH2Cl2 as solvent,sodium bicarbonate as acid binding reagent,n(diphenyl ether)∶n(ethyl pyruvate)∶n(AlCl3)=1.4∶1.0∶1.2,the yield of ethyl 2-(4-phenoxyphenyl)lactate was 86.2%.The structure of target compound was characterized by IR and 1H NMR.
出处
《化学世界》
CAS
CSCD
北大核心
2012年第10期610-611,621,共3页
Chemical World