通过有机硼酸盐和有机双(硼酸盐)的分子内胺化反应构建氮杂环。
Construction of Azacycles by Intramolecular Amination of Organoboronates and Organobis(boronates).
机构信息
Department of Chemistry, Merkert Chemistry Center, Boston College, Chestnut Hill, Massachusetts 02467, United States.
Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States.
出版信息
Org Lett. 2021 May 7;23(9):3379-3383. doi: 10.1021/acs.orglett.1c00856. Epub 2021 Apr 14.
PMID:33852313
Abstract
Intramolecular amination of organoboronates occurs with a 1,2-metalate shift of an aminoboron "ate" complex to form azetidines, pyrrolidines, and piperidines. Bis(boronates) undergo site-selective amination to form boronate-containing azacycles. Enantiomerically enriched azacycles are formed with high stereospecificity.
摘要
硼酸酯的分子内胺化反应伴随着氨基硼“ate”配合物的 1,2-金属迁移，形成氮杂环丁烷、吡咯烷和哌啶。双（硼酸酯）发生选择性胺化反应，形成含硼酸酯的氮杂环。手性富集的氮杂环可以高立体特异性形成。
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