摘要
手性1,2-二(2-甲氧基苯基)-1,2-乙二胺可作为有机小分子催化剂、金属配体前体广泛应用于多种有机合成反应之中,其可以消旋体为原料通过拆分得到。以廉价易得的邻甲氧基苯甲醛为原料,重点针对亚胺中间体还原过程中反应条件苛刻、后处理复杂等问题,首次利用Mg作为还原剂,在室温下,以93%的分离收率得到关键中间体3。通过该关键步骤的放大实验(92%),进一步评价了该方法的应用潜力。
As a key organic small molecule catalyst and ligand precursors in metal catalysis,chiral 1,2-bis(2-methoxyphenyl)-1,2-ethylenediamine can be applied in various organic synthesis reactions,which can be obtained through racemic resolution.Typically,reduction of imine intermediate exhibited the problem of harsh reaction conditions.Here,cheap o-methoxybenzaldehyde was used as raw material and Mg was used as reducing agent.The key intermediate 3 could be obtained with 93%isolated yield under ambient temperature.Meanwhile,through the large-scale experiment of the key step(92%),the industrial application potential of the method is further evaluated.
作者
邸相杰
邹胜
黄晴菲
范挺
王启卫
DI Xiang-jie;ZOU Sheng;HUANG Qing-fei;FAN Ting;WANG Qi-wei(Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China;University of Chinese Academy of Sciences, Beijing 100049, China)
出处
《合成化学》
CAS
2021年第4期315-319,共5页
Chinese Journal of Synthetic Chemistry
基金
中国科学院“西部之光”人才培养计划。
