Achieving versatile Cu-catalyzed multicomponent 1,1-aminosilylation reactions from feedstock reagents

08 April 2025, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

1,1-aminosilanes are emerging as valuable reagents for diversification efforts while also showing potential for silicon-based drug develop-ment. However, no strategies exist to access broad libraries of structurally and electronically diverse1,1-aminosilanes from readily available materials. Herein, we disclose a Cu-catalyzed multicomponent reaction for the direct synthesis of 1,1-aminosilanes from simple feedstock chemicals. This method provides a high yielding, cost-effective, operationally simple, and scalable approach with broad functional group tolerance. Compatible with both aliphatic and aromatic aldehydes as well as primary and secondary amines, it also enables late-stage modifications of FDA approved drugs and their precursors, unlocking new opportunities in pharmaceutical and materials science.

Keywords

multicomponent
coupling
aminosilylation
difunctionalization

Supplementary materials

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Detailed experimental procedures, characterization data, and NMR spectra for all new compounds.
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