A Facile Epoxide Aminolysis Promoted by (t-BuO)(2)Mg and Its Application to the Synthesis of Efinaconazole
文献类型：期刊论文
| 作者 | Zhu, Fuqiang1,2; Xie, Yuanchao3; Zhang, Jian4; Tian, Guanghui4; Qin, Hongjian4; Yang, Xiaojun4; Hu, Tianwen4; He, Yang3; Aisa, Haji A.2; Shen, Jingshan3
|
| 刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT
 |
| 出版日期 | 2018-05 |
| 卷号 | 22期号:5页码:625-632 |
| ISSN号 | 1083-6160 |
| DOI | 10.1021/acs.oprd.8b00081 |
| 文献子类 | Article |
| 英文摘要 | 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)(2)Mg. The desired beta-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. |
| WOS关键词 | ASYMMETRIC-SYNTHESIS ; 1,2-AMINO ALCOHOLS ; ANTIFUNGAL AGENTS ; EFFICIENT ; DERIVATIVES ; MILD ; ONYCHOMYCOSIS ; CATALYSTS ; BROMIDE ; DESIGN |
| 资助项目 | National Science Foundation for Young Scientists of China[21502209] ; Topharman Shandong Ltd.[00000000] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000432901100007 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279775]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Aisa, Haji A.; Shen, Jingshan |
| 作者单位 | 1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; 2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, South Beijing Rd 40-1, Urumqi 830011, Xinjiang, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 4.Topharman Shanghai Co Ltd, Bldg 1,388 Jialilue Rd,Zhangjiang Hitech Pk, Shanghai 201209, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhu, Fuqiang,Xie, Yuanchao,Zhang, Jian,et al. A Facile Epoxide Aminolysis Promoted by (t-BuO)(2)Mg and Its Application to the Synthesis of Efinaconazole[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2018,22(5):625-632. |
| APA | Zhu, Fuqiang.,Xie, Yuanchao.,Zhang, Jian.,Tian, Guanghui.,Qin, Hongjian.,...&Shen, Jingshan.(2018).A Facile Epoxide Aminolysis Promoted by (t-BuO)(2)Mg and Its Application to the Synthesis of Efinaconazole.ORGANIC PROCESS RESEARCH & DEVELOPMENT,22(5),625-632. |
| MLA | Zhu, Fuqiang,et al."A Facile Epoxide Aminolysis Promoted by (t-BuO)(2)Mg and Its Application to the Synthesis of Efinaconazole".ORGANIC PROCESS RESEARCH & DEVELOPMENT 22.5(2018):625-632. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。