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Updated: Jul 3, 2025

Versatile CO2 Transformations into Complex Products: A One-pot Two-step Strategy
Published on: November 9, 2019
Simplified Version of the Eschweiler-Clarke Reaction
Klim O Biriukov1, Evgeniya Podyacheva1,2, Ignatii Tarabrin3
1A. N. Nesmeyanov Institute of Organoelement Compounds of Russian Academy of Sciences, Vavilova St. 28, bld. 1, INEOS, 119334 Moscow, Russia.
Abstract:
The traditional Eschweiler-Clarke reaction is a three-component process involving formaldehyde, amine, and formic acid. In this work, we showed that the reductive potential of formaldehyde was sufficient to provide methylation of secondary amines in the absence of acidic additives. Various acid-sensitive moieties remain intact under developed conditions. The scalability of the elaborated approach was shown for several products. Synthesis of the antifungal agent butenafine demonstrated the preparative utility of the developed approach.
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