氨解
环氧化物
材料科学
化学
有机化学
催化作用
作者
Fuqiang Zhu,Yuanchao Xie,Jian Zhang,Guanghui Tian,Qin Hongjian,Xiaojun Yang,Tianwen Hu,Yang He,Haji Akber Aisa,Jingshan Shen
标识
DOI:10.1021/acs.oprd.8b00081
摘要
A novel and efficient method for the aminolysis of trizole epoxides is described. This method consists of a facile ring opening of the epoxides mediated by t-BuOMgCl generated in situ from amine hydrochlorides and (t-BuO)2Mg. The desired β-amino alcohols were obtained in good yields without employing other heavy metals or precious catalysts. The optimized conditions were successfully applied to the synthesis of a number of potential triazole antifungal compounds as well as efinaconazole on up to a 700 g scale.
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