Rapid Assembly of Saturated Nitrogen Heterocycles in One-Pot: Diazo-Heterocycle '˜Stitching'™ by N-H Insertion and Cyclization

Alexander Boddy
Methods that provide rapid access to new heterocyclic structures in biologically relevant chemical space provide important opportunities in drug discovery. Here, a strategy is described for the preparation of 2,2-disubstituted azetidines, pyrrolidines, piperidines and azepanes bearing ester and diverse aryl substituents. A one-pot rhodium catalyzed NâH insertion and cyclization sequence uses diazo compounds to stitch together linear 1,m-haloamines (m = 2 to 5) to rapidly assemble 4-, 5-, 6- and 7-membered saturated nitrogen heterocycles in...
2 citations reported since publication in 2018.
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