A hybrid chemoenzymatic protocol for the stereoselective preparation of chiral 2-substituted azacycles is reported. Our methodology relies on a cyclization/bioreduction sequence promoted by organolithium reagents and imine reductase (IRED) enzymes, working under air and at room temperature, with three consecutive C–C/C–N/C–H bond formation events occurring in a one-pot, telescoped synthetic operation.
When organolithiums meet imine reductases: a hybrid chemoenzymatic route towards chiral N-heterocycles
Meazzo, CarolinaFirst
;De Nardi, Federica;Parisotto, Stefano;Blangetti, Marco
;Prandi, Cristina
2026-01-01
Abstract
A hybrid chemoenzymatic protocol for the stereoselective preparation of chiral 2-substituted azacycles is reported. Our methodology relies on a cyclization/bioreduction sequence promoted by organolithium reagents and imine reductase (IRED) enzymes, working under air and at room temperature, with three consecutive C–C/C–N/C–H bond formation events occurring in a one-pot, telescoped synthetic operation.
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