Tandem Cu(I)-Catalyzed Dipolar Cycloaddition-C-H Activation for the In-Flow Synthesis of N-Pyridyl-5-amino-1,2,3-triazole-4-carboxylates

A telescoped process under continuous flow conditions has been developed for the synthesis of N-pyridyl-5-amino-1,2,3-triazole-4-carboxylate derivatives, catalyzed by copper salts in a packed bed reactor. The approach is initiated by the application of click chemistry, wherein a Cu(I)-catalyzed 1,3-dipolar azide–alkyne cycloaddition (CuAAC) is employed to enable the efficient and selective formation of a triazole ring. This is followed by a copper-mediated C–H activation step, through which an inert C–H bond is replaced with a C–N bond. Through this strategy, an environmentally acceptable and cost-effective method for the synthesis of highly functionalized organic molecules is provided.

• Donato, E
• Mayorquín-Torres, MC
• Puglisi, A
• Benaglia, M
• Adamo, MFA
• Stevens, CV

• Dipartimento di Chimica, Università degli Studi di Milano, 20133 Milano, Italy

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