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钯催化的C-H活化/分子内胺化反应:一种合成3-芳基/烷基吲唑的新途径。

Palladium-catalyzed C-H activation/intramolecular amination reaction: a new route to 3-aryl/alkylindazoles.

作者信息

Inamoto Kiyofumi, Saito Tadataka, Katsuno Mika, Sakamoto Takao, Hiroya Kou

机构信息

Graduate School of Pharmaceutical Sciences, Tohoku University, 6-3, Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan.

出版信息

Org Lett. 2007 Jul 19;9(15):2931-4. doi: 10.1021/ol0711117. Epub 2007 Jun 27.

Abstract

A method for the catalytic C-H activation of hydrazone compounds followed by intramolecular amination is described. It requires the use of a catalytic amount of Pd(OAc)2 in the presence of Cu(OAc)2 and AgOCOCF3, which efficiently effects the cyclization to afford variously substituted indazoles. The reactions proceed under relatively mild conditions and thus tolerate a variety of functional groups, including alkoxycarbonyl and cyano groups and halogen atoms.

摘要

描述了一种腙化合物的催化C-H活化随后进行分子内胺化的方法。该方法需要在Cu(OAc)₂和AgOCOCF₃存在下使用催化量的Pd(OAc)₂,其能有效地实现环化反应,得到各种取代的吲唑。反应在相对温和的条件下进行,因此能耐受包括烷氧羰基、氰基和卤素原子在内的多种官能团。

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