Donato Emanuela, Mayorquín-Torres Martha C, Puglisi Alessandra, Benaglia Maurizio, Adamo Mauro F A, Stevens Christian V
Dipartimento di Chimica, Università degli Studi di Milano, 20133 Milano, Italy.
Department of Green Chemistry and Technology, Ghent University, B-9000 Ghent, Belgium.
Org Lett. 2025 May 2;27(17):4423-4427. doi: 10.1021/acs.orglett.5c00453. Epub 2025 Apr 18.
A telescoped process under continuous flow conditions is described for the synthesis of -pyridyl-5-amino-1,2,3-triazole-4-carboxylate derivatives catalyzed by copper salts in a packed bed reactor. The synthetic approach takes first advantage of click chemistry, specifically relying on Cu(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition (CuAAC), to achieve the efficient and selective assembly of a triazole ring, followed by a copper-mediated C-H activation, that substitutes an inert C-H bond with a C-N bond, providing an environmentally acceptable and cost-effective strategy for synthesizing highly functionalized organic molecules.
描述了一种在连续流动条件下的 telescoped 过程，用于在填充床反应器中由铜盐催化合成 -吡啶基-5-氨基-1,2,3-三唑-4-羧酸盐衍生物。该合成方法首先利用点击化学，特别是依靠铜（I）催化的 1,3-偶极叠氮化物-炔烃环加成反应（CuAAC）来实现三唑环的高效和选择性组装，随后进行铜介导的 C-H 活化，即将惰性 C-H 键用 C-N 键取代，为合成高度官能化的有机分子提供了一种环境友好且具有成本效益的策略。
