4.5 Article

Enantioselective Synthesis of 2-Substituted Pyrrolidines via Intramolecular Reductive Amination

Journal

SYNTHESIS-STUTTGART
Volume 51, Issue 13, Pages 2713-2719

Publisher

GEORG THIEME VERLAG KG
DOI: 10.1055/s-0037-1611533

Keywords

asymmetric catalysis; intramolecular reductive amination; iridium; chiral ligand; arylpyrrolidine

Funding

  1. National Natural Science Foundation of China [21772155, 21402155, 21602172]

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Catalyzed by the complex generated in situ from iridium and the chiral ferrocene ligand, tert -butyl (4-oxo-4-arylbutyl)carbamate substrates were deprotected and then reductively cyclised to form 2-substituted arylpyrrolidines in a one-pot manner, in which the intramolecular reductive amination was the key step. A range of chiral 2-substituted arylpyrrolidines were synthesised in up to 98% yield and 92% ee .

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