PhI(OPiv)2/氟化氢-吡啶体系介导的无金属的烯烃分子内氨基氟化反应。
Metal-free intramolecular aminofluorination of alkenes mediated by PhI(OPiv)2/hydrogen fluoride-pyridine system.
机构信息
The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
出版信息
Org Biomol Chem. 2012 Nov 21;10(43):8566-9. doi: 10.1039/c2ob26664d.
PMID:23007735
Abstract
A convenient, metal-free intramolecular aminofluorination of alkenes has been developed. Employing readily available PhI(OPiv)(2) and hydrogen fluoride-pyridine in the presence of BF(3)·OEt(2), tosyl-protected pent-4-en-1-amines were converted to 3-F-piperidines in one step in good yields as well as high stereoselectivity.
摘要
一种方便、无金属的烯烃分子内氨基氟化方法已经被开发出来。在 BF(3)·OEt(2)的存在下，使用易得的 PhI(OPiv)(2)和氟化氢-吡啶，对甲苯磺酰基保护的戊-4-烯-1-胺可以一步转化为 3-F-哌啶，产率高，立体选择性好。
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