新型N-苄基苯甲酰胺衍生物的合成

摘要

With substitutional benzoic acid as raw material,synthetic strategy was completed by chlorina-tion and acyl reaction with 2-amino-1-phenylethanol in alkaline system, five novel chalcone derivatives (3a~3e) were synthesized,and the structures were characterized by 1 H NMR and ESI-MS. The effects of acid-binding agents,reaction temperature and time on yield were investigated. The results show that the better reaction conditions of the acyl reaction are as follows:triethylamine is acid-binding agents,the reac-tion temperature is 0 ℃,the reaction time is 2 h,and the acyl reaction yield can reach more than 50%.%以取代的苯甲酸为原料,经氯代反应生成对应的酰氯,然后在碱性条件下与2-苯氨基乙醇反应得到5个新型的具有N-苄基苯甲酰胺结构的化合物(3a~3e),并采用1H NMR和ESI-MS对其结构进行了表征。考察了酰化反应中缚酸剂、时间、温度等因素对不同取代基的酰化反应收率的影响。结果表明,酰化反应的较佳条件是：三乙胺为缚酸剂,反应温度0℃,反应时间2 h,酰化反应收率达50%以上。