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A Facile Epoxide Aminolysis Promoted by (t-BuO)(2)Mg and Its Application to the Synthesis of Efinaconazole
Zhu, FQ (Zhu, Fuqiang); Xie, YC (Xie, Yuanchao); Zhang, J (Zhang, Jian); Tian, GH (Tian, Guanghui); Qin, HJ (Qin, Hongjian); Yang, XJ (Yang, Xiaojun); Hu, TW (Hu, Tianwen); He, Y (He, Yang); Aisa, HA (Aisa, Haji A.); Shen, JS (Shen, Jingshan)
2018
Source PublicationORGANIC PROCESS RESEARCH & DEVELOPMENT
ISSN1083-6160
Volume22Issue:5Pages:625-632
Abstract

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.

DOI10.1021/acs.oprd.8b00081
Indexed BySCI
WOS IDWOS:000432901100007
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Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/5409
Collection省部共建新疆特有药用资源利用重点实验室
资源化学研究室
Corresponding AuthorAisa, HA (Aisa, Haji A.)
Affiliation1.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
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.Topharman Shanghai Co Ltd, Bldg 1,388 Jialilue Rd,Zhangjiang Hitech Pk, Shanghai 201209, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
Recommended Citation
GB/T 7714
Zhu, FQ ,Xie, YC ,Zhang, J ,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, FQ .,Xie, YC .,Zhang, J .,Tian, GH .,Qin, HJ .,...&Shen, JS .(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, FQ ,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.
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