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一种以二氯甲烷为亚甲基源的芳香胺甲基化的有效方法。

An Efficient Approach to Aromatic Aminomethylation Using Dichloromethane as Methylene Source.

作者信息

Ostacolo Carmine, Di Sarno Veronica, Musella Simona, Ciaglia Tania, Vestuto Vincenzo, Pepe Giacomo, Merciai Fabrizio, Campiglia Pietro, Gomez Monterrey Isabel M, Bertamino Alessia

机构信息

Department of Pharmacy, University of Naples "Federico II", Naples, Italy.

Department of Pharmacy, University of Salerno, Fisciano, Italy.

出版信息

Front Chem. 2019 Aug 13;7:568. doi: 10.3389/fchem.2019.00568. eCollection 2019.

Abstract

Ultrasound-promoted N-aminomethylation of indoles can be achieved in basic medium using sodium hydride and dichloromethane (DCM) as C1 donor source. This innovative amino methylation protocol results in good to excellent yields of multifunctional indole derivatives. The procedure is also applicable to other aza-heterocyclic compounds and, interestingly, affords direct access to aminomethyl-substituted aryl alcohols.

摘要

在碱性介质中,以氢化钠和二氯甲烷(DCM)作为C1供体源,可实现超声促进的吲哚N-氨甲基化反应。这种创新的氨甲基化方法可得到产率良好至优异的多功能吲哚衍生物。该方法也适用于其他氮杂环化合物,有趣的是,还能直接得到氨甲基取代的芳基醇。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0929/6700257/b136f5ec1d14/fchem-07-00568-g0001.jpg

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