由2-甲酰基苯硼酸合成吲唑类化合物。

Solomin Vitalii V, Seins Alberts, Jirgensons Aigars

Latvian Institute of Organic Synthesis Aizkraukles 21 Riga LV-1006 Latvia

Faculty of Materials Science and Applied Chemistry, Riga Technical University P. Valdena Str. 3 Riga LV-1048 Latvia.

RSC Adv. 2021 Jun 28;11(37):22710-22714. doi: 10.1039/d1ra04056a. eCollection 2021 Jun 25.

A method for the synthesis of indazoles was developed which involves a copper(ii) acetate catalysed reaction of 2-formylboronic acids with diazadicaboxylates followed by acid or base induced ring closure. Hydrazine dicarboxylates were also shown as competent reaction partners for the synthesis of indazoles, however, they required a stoichiometric amount of copper(ii) acetate for the C-N bond formation step. The transformation can be efficiently performed as a two step-one pot procedure to give a range of 1-alkoxycarbonyl indazoles.

开发了一种合成吲唑的方法，该方法涉及醋酸铜（II）催化的2-甲酰基硼酸与重氮二羧酸盐的反应，然后进行酸或碱诱导的环化反应。肼二羧酸盐也被证明是合成吲唑的有效反应伙伴，然而，在C-N键形成步骤中，它们需要化学计量的醋酸铜（II）。该转化反应可以有效地以两步一锅法进行，以得到一系列1-烷氧羰基吲唑。