首页|Pd-有机膦催化Suzuki偶联合成2-氨基-5-氟-3',4'-二氯联苯

Pd-有机膦催化Suzuki偶联合成2-氨基-5-氟-3',4'-二氯联苯

扫码查看
以3,4-二氯苯硼酸和2-溴-4-氟苯胺为原料,在碱性条件下使用Pd-有机膦复合催化剂进行Suzuki偶联反应,经分液、减压浓缩得到2-氨基-5-氟-3',4'-二氯联苯.通过对不同反应条件进行优化,获得优化条件为:以甲苯和水为混合溶剂,n(2-溴-4-氟苯胺)∶n(3,4-二氯苯硼酸)∶n(K2CO3)∶n(复合催化剂)=1∶1.2∶1.2∶0.000 5,反应温度85 ℃,反应时间4 h,产物纯度98.0%,收率大于97.0%.该方法催化剂用量少、工艺简单、产品收率高,符合绿色化学生产理念,具有工业化前景.
Synthesis of 2-Amino-5-fluoro-3',4'-dichlorobiphenyl by Suzuki Coupling Catalyzed by Pd-organophosphine
Using 3,4-dichlorophenylboronic acid and 2-bromo-4-fluoroaniline as raw materials,a Pd-organophosphine composite catalyst was used for Suzuki coupling reaction under alkaline conditions,and 2-amino-5-fluoro-3'4'-dichlorobiphenyl was obtained after separation and reduced pressure concentration.The results under different reaction conditions were analyzed,and the optimized conditions were:toluene and water as mixed solvents,n(2-bromo-4-fluoroaniline)∶n(3,4-dichlorophenylboronic acid)∶n(K2CO3)∶n(composite catalyst)=1∶1.2∶1.2∶0.000 5,the reaction temperature was 85 ℃,the reaction time was 4 h,the purity was 98.0%,and the yield was greater than 97.0%.The method requires less catalyst,has a simple process,and has a high product yield.It conforms to the concept of green chemical production and has industrial prospects.

2-amino-5-fluoro-3',4'-dichlorobiphenylPd-organophosphineBixafenSuzuki coupling reaction

王振州、竺来发、尤瑶瑶、吴曼、曹金艳、陈灿、成鸿静

展开 >

湖南化工研究院有限公司 国家农药创制工程技术研究中心,湖南长沙 410014

农用化学品湖南省重点实验室,湖南长沙 410014

2-氨基-5-氟-3',4'-二氯联苯 Pd-有机膦 联苯吡菌胺 Suzuki偶联反应

2024

精细化工中间体
湖南化工研究院

精细化工中间体

CSTPCD
影响因子:0.236
ISSN:1009-9212
年,卷(期):2024.54(6)