A New Catalytic Cross-Coupling
Approach for the Synthesis of Protected
Aryl and Heteroaryl Amidines

Neumann, William L.

A New Catalytic Cross-Coupling Approach for the Synthesis of Protected Aryl and Heteroaryl Amidines

Posted on 2002-02-19 - 00:00

A new method for the synthesis of protected benzamidines is described. The commercially available 1,3-bis(tert-butoxycarbonyl)-2-methyl-2-thiopseudourea guanidylation reagent, after SEM-protection, functions as an amidine-forming cross-coupling partner under Liebeskind−Srogl conditions. In the presence of copper(I) thiophenecarboxylate (CuTC), the palladium-catalyzed cross-coupling of the SEM-protected thiopseudourea reagent with boronic acids affords fully protected benzamidines in good to excellent yield (40−91%).

CITE THIS COLLECTION

Kusturin, Carrie L.; Liebeskind, Lanny S.; Neumann, William L. (2016). A New Catalytic Cross-Coupling Approach for the Synthesis of Protected Aryl and Heteroaryl Amidines. ACS Publications. Collection. https://doi.org/10.1021/ol025547s

https://doi.org/10.1021/ol025547s

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