2-氨基苯甲酰胺衍生物的合成与应用  

Synthesis and Application of 2-Aminobenzamide Derivatives

作　　者：杨莎[1] 李晓花[1] 杜漠 高艳蓉 朱周静 唐文强 YANG Sha;LI Xiaohua;DU Mo;GAO Yanrong;ZHU Zhoujing;TANG Wenqiang(School of Pharmacy,Shaanxi Institute of International Trade&Commerce,Xianyang 712046,China;Xianyang Key Laboratory of Molecular Imaging and Drug Synthesis,Xianyang 712046,China)

机构地区：[1]陕西国际商贸学院医药学院,陕西咸阳712046 [2]咸阳市分子影像与药物合成重点实验室,陕西咸阳712046

出　　处：《化学与生物工程》2024年第4期60-63,共4页Chemistry & Bioengineering

基　　金：咸阳市分子影像与药物合成重点实验室项目(2021QXNL-PT-0008)。

摘　　要：以2-氨基苯甲腈衍生物(2a~2f)为原料,在氢氧化钾碱性条件下发生水解反应合成了2-氨基苯甲酰胺衍生物(1a~1f),对合成条件进行了优化,通过1 HNMR对产物结构进行了表征。结果表明,在氢氧化钾用量n(KOH)∶n(2a)为4∶1、回流反应14 h的最佳条件下,衍生物1a的收率达到84%;以多聚磷酸为催化剂,衍生物1a与苯甲醛在微波辅助下可以合成7-甲基-2-苯基-2,3-二氢喹唑啉-4(1 H)-酮(3)。Using 2-aminobenzonitrile derivatives(2a-2f)as raw materials,we synthesized 2-aminobenzamide derivatives(1a-1f)through hydrolysis reaction under alkaline conditions of potassium hydroxide.Moreover,we optimized the synthesis conditions and characterized the structure of the product by 1 HNMR.The results show that the yield of derivative 1a reaches 84%under the optimal conditions as follows:potassium hydroxide dosage n(KOH)∶n(2a)of 4∶1,reaction at refluxing temperature for 14 h.Using polyphosphoric acid as a catalyst,7-methyl-2-phenyl-2,3-dihydroquinazolin-4(1 H)-one(3)can be synthesized from derivative 1a and benzaldehyde via microwave-assisted method.

关 键 词：2-氨基苯甲酰胺 水解反应 工艺优化 

分 类 号：TQ463[化学工程—制药化工]