New methods for the synthesis of alkylamines

Alkylamines are ubiquitous motifs in medicines, pre-clinical candidates, biological probes, agrochemicals & functional materials. Amine functionality has the potential to bind to proteins due to its capacity to form donor/acceptor hydrogen bonds. Furthermore, upon protonation, the solubility and the bioavailability of the dugs containing amine motifs can be enhanced. Accordingly, alkylamines appear in approx. 35% of pharmaceuticals, and around 60% contain a tertiary alkylamine. Therefore, the need to access alkylamine scaffolds drives the continued development of general methods for their synthesis. The method of choice is typically reductive amination, wherein a carbonyl is condensed with a alkylamine to form an iminium, whose reduction leads to a higher order. Although widely employed, the development of new processes for the construction of complex systems is essential to achieve significant impact on the synthesis. Systematic methods for the synthesis of complex alkylamines would be valuable to the pharmaceutical, agrochemical and fine chemicals industries.




















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