Qian X.; Zhou, H.; Chaminda Lakmal, H. H.; Lucore, J. (undergraduate researcher); Wang, X.; Valle, U. H.; Donnadieu, B.; Xu X.; Cui X.* “Fe(III)-Based Tandem Catalysis for Amidomethylative Multiple Substitution Reactions of α-Substituted Styrene Derivatives” ACS Catal. 2020, 10, 10627.
The Cui group has developed a set of new pathways to perform tandem catalysis, which enabled direct access to several types of pharmaceutically important building blocks from simple alkenes. Using simple Fe(III) catalyst, multiple amidomethylative C–H substitution events around the C=C bonds of commodity alkenes have been developed to rapidly install functional groups while reserving the unsaturation. The operationally simple protocols employ bench-stable bisamidomethane as the sole reagent, producing hexahydropyrimidine and 1,2,3,6-tetrahydropyridine derivatives, two classes of N-heterocycles that are key units in many drug molecules. From simple α-methylstyrenes, the catalytic processes have been further applied for rapid access to a broader scope of synthetic building blocks, including unsaturated 1,3-diamine and bispidine derivatives.
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