4-环丙基氨基甲酰-苯硼酸合成工艺优化

Optimization of Synthesis Process of 4-cyclopropyl Carbamyl-benzoboric Acid

4-环丙基氨基甲酰-苯硼酸是合成多种具有药物活性分子的重要中间体,而且在生物学、医学及材料科学中有着广泛的应用。该研究以对苯硼酸为起始原料,以DCM作为溶剂,加入DMF和次氯酸,经过酰化反应得到底物1,再与以KCO 3作为缚酸剂中和掉体系中的酸,在DCM中发生胺化反应,合成得到目标化合物,其结构经MS和1H NMR确证。该方法简单、原料廉价易得、操作简便易控且收率较高,反应总收率为78%。

4-cyclopropylcarbamoyl-phenylboronic acid is an important intermediate for the synthesis of a variety of pharmacologically active molecules,and it has a wide range of applications in biology,medicine,and materials science.The p-phenylboronic acid was used as the starting material,DCM was used as the solvent,DMF and hypochlorous acid were added,and the substrate 1 was obtained through the acylation reaction,and then the acid in the system was neutralized with KCO 3 as the acid binding agent.Amination reaction occurred in the synthesis to obtain the target compound,the structure of which was confirmed by MS and 1H NMR.The method was simple,the raw materials erre cheap and easy to obtain,the operation was simple and easy to control,and the yield was high.The total reaction yield was 78%.