Published November 4, 2019 | Version v1
Journal article

Enantioselective rhodium-catalyzed addition of arylboroxines to N-unprotected ketimines: Efficient synthesis of cipargamin

  • 1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology (China)
  • 2. State Key Laboratory of Bio-Organic and Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)

Description

Highly enantioselective rhodium-catalyzed addition of arylboroxines to N-unprotected ketimines is realized for the first time by employing chiral BIBOP-type ligands with a Rh loading as low as 1 mol %. A range of chiral α-trifluoromethyl-α,α-diaryl α-tertiary amines or 3-amino-3-aryloxindoles were formed with excellent ee values and yields by employing either WingPhos or PFBO-BIBOP as the ligand. The method has enabled an efficient enantioselective synthesis of cipargamin. (© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim)

Availability note (English)

Available from: http://dx.doi.org/10.1002/anie.201910008

Additional details

Identifiers

Publishing Information

Journal Title
Angewandte Chemie (International Edition)
Journal Volume
58
Journal Issue
45
Journal Page Range
p. 16119-16123
ISSN
1433-7851
CODEN
ACIEF5