Automated One-Pot Library Synthesis with Aldehydes as Radical Precursors

Abstract

The increased demand for the synthesis of Csp³ enriched motifs and the urgency of discovering new drugs requires the development of more efficient technologies and synthetic tools to accelerate drug discovery processes. Herein, we report a fully automated strategy for the addition of Csp³ enriched building blocks onto olefins via Giese addition to forge Csp³−Csp³ bonds. The developed fully automated protocol allowed the in-situ conversion of aldehydes (non-redox-active species) to electroactive imidazolidines and their use as precursors of C-centered radicals under photoredox catalyzed conditions for the synthesis of building blocks and bioactive compound libraries by synthesizing sp³-enriched compounds.