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Issue 6, 2012
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Catalytic asymmetric α-amination of carboxylic acids using isothioureas

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Abstract

HBTM-2.1 promotes the direct asymmetric α-amination of carboxylic acids with N-aryl-N-aroyldiazenes at low catalyst loadings (as low as 0.25 mol%), giving either 1,3,4-oxadiazin-6-ones or N-protected α-amino acid derivatives (upon ring opening) with exquisite enantiocontrol (typically ≥99% ee).

Graphical abstract: Catalytic asymmetric α-amination of carboxylic acids using isothioureas

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Article information


Submitted
09 Feb 2012
Accepted
07 Mar 2012
First published
08 Mar 2012

Chem. Sci., 2012,3, 2088-2093
Article type
Edge Article

Catalytic asymmetric α-amination of carboxylic acids using isothioureas

L. C. Morrill, T. Lebl, A. M. Z. Slawin and A. D. Smith, Chem. Sci., 2012, 3, 2088
DOI: 10.1039/C2SC20171B

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